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Pictilisib (GDC-0941) PI3Kα/δ Inhibitor

Name: Pictilisib (GDC-0941)
Brand: Selleck Chemicals
SKU: S1065
Availability: InStock
Rating: 5 (435 reviews)

Cat.No.S1065

Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.

Chemical Structure

Molecular Weight: 513.64

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other PI3K Inhibitors	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Sf9	Kinase Assay		1 h	DMSO	Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM	18754654
Sf9	Kinase Assay		1 h	DMSO	Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM	18754654
Sf9	Kinase Assay		1 h	DMSO	Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM	18754654
Sf9	Kinase Assay		1 h	DMSO	Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.033 μM	18754654
Sf9	Kinase Assay		1 h	DMSO	Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha	18754654
MDA-MB-361	Function Assay		2 h	DMSO	Inhibition of Akt Ser473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.028 μM	18754654
PC3	Function Assay		2 h	DMSO	Inhibition of Akt Ser473 phosphorylation in PTEN-null human PC3 cells with IC50 of 0.037 μM	18754654
U87MG	Function Assay		2 h	DMSO	Inhibition of Akt Ser473 phosphorylation in PTEN-null human U87MG cells with IC50 of 0.046 μM	18754654
MDA-MB-361	Growth Inhibition Assay		96 h	DMSO	Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.72 μM	18754654
A2780	Growth Inhibition Assay		96 h	DMSO	Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation with IC50 of 0.14 μM	18754654
PC3	Growth Inhibition Assay		96 h	DMSO	IC50=0.28 μM	18754654
U87MG	Growth Inhibition Assay		96 h	DMSO	IC50=0.95 μM	18754654
Sf9	Kinase Assay		30 min	DMSO	Inhibition of human PI3Kgamma expressed assessed as amount of ATP consumed with IC50 of 0.042 μM	22548342
RAW 264.7	Kinase Assay		90 min	DMSO	Inhibition of human PI3Kgamma expressed assessed as inhibition of AKT phosphorylation with IC50 of 0.298 μM	22548342
Sf9	Kinase Assay		1 h		Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells with IC50 of 0.017 μM	23540645
Sf9	Kinase Assay		1 h		Inhibition of GST-fused human recombinant PI3Kdelta expressed	23540645
Sf9	Kinase Assay		1 h		Inhibition of GST-fused human recombinant PI3Kgamma expressed	23540645
Sf9	Kinase Assay		1 h		Inhibition of GST-fused human recombinant PI3Kalpha expressed	23540645
SKOV3	Kinase Assay	1 μM	1 h	DMSO	Inhibition of PI3Kalpha assessed as inhibition of Akt Ser473 phosphorylation	23360348
MCF7	Growth Inhibition Assay	1 μM	96 h	DMSO	GI50=0.0702 μM	23360348
SKOV3	Growth Inhibition Assay	1 μM	96 h	DMSO	GI50=0.1476 μM	23360348
PC3	Growth Inhibition Assay		72 h	DMSO	IC50=0.28 μM	21981714
MCF7.1	Growth Inhibition Assay		72 h	DMSO	Antiproliferative activity against human MCF7.1 cells expressing HER2 gene with IC50 of 0.28 μM	21981714
MCF7-neo/Her2	Growth Inhibition Assay		72 h	DMSO	IC50=0.29 μM	23662903
MCF7-neo/Her2	Kinase Assay				Inhibition of PI3Kalpha assessed as reduction of AKT phosphorylation at S473 with IC50 of 0.007 μM	23662903
PC3	Growth Inhibition Assay		72 h	DMSO	EC50=0.34 μM	21985639
MCF7.1	Growth Inhibition Assay		72 h	DMSO	Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with EC50 of 0.39 μM	21985639
PC3	Growth Inhibition Assay		72 h	DMSO	Antiproliferative activity against human PC3 cells deficient in PTEN with IC50 of 0.39 μM	20050669
MCF7.1	Growth Inhibition Assay		72 h	DMSO	Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with IC50 of 0.34 μM	20050669
MCF7.1	Growth Inhibition Assay		72 h		EC50=0.72 μM	20346656
NCI-H1975	Cytotoxic Assay		72 h		IC50=0.27 μM	23059545
H460	Cytotoxic Assay		72 h		IC50=0.87 μM	23059545
HT-29	Cytotoxic Assay		72 h		IC50=0.66 μM	23059545
HepG2	Cytotoxic Assay		72 h		IC50=1 μM	23059545
SGC7901	Cytotoxic Assay		72 h		IC50=1.8 μM	23059545
NCI-H226	Cytotoxic Assay		72 h		IC50=2.9 μM	23059545
A549	Cytotoxic Assay		72 h		IC50=6.9 μM	23059545
U87MG	Cytotoxic Assay		72 h		IC50=7.77 μM	23059545
HBC4	Growth Inhibition Assay				logGI50=-6.03 M	22336246
BSY1	Growth Inhibition Assay				logGI50=-6.90 M	22336246
HBC5	Growth Inhibition Assay				logGI50=-6.60 M	22336246
MCF7	Growth Inhibition Assay				logGI50=-7.33 M	22336246
MDA-MB-231	Growth Inhibition Assay				logGI50=-5.46 M	22336246
U251	Growth Inhibition Assay				logGI50=-5.50 M	22336246
SF268	Growth Inhibition Assay				logGI50=-5.39 M	22336246
SF295	Growth Inhibition Assay				logGI50=-6.37 M	22336246
SF539	Growth Inhibition Assay				logGI50=-6.50 M	22336246
SNB75	Growth Inhibition Assay				logGI50=-7.10 M	22336246
SNB78	Growth Inhibition Assay				logGI50=-6.52 M	22336246
HCC2998	Growth Inhibition Assay				logGI50=-6.29 M	22336246
KM12	Growth Inhibition Assay				logGI50=-5.76 M	22336246
HT-29	Growth Inhibition Assay				logGI50=-6.30 M	22336246
HCT15	Growth Inhibition Assay				logGI50=-6.12 M	22336246
HCT116	Growth Inhibition Assay				logGI50=-5.87 M	22336246
NCI-H23	Growth Inhibition Assay				logGI50=-5.73 M	22336246
NCI-H226	Growth Inhibition Assay				logGI50=-6.21 M	22336246
NCI-H522	Growth Inhibition Assay				logGI50=-6.58 M	22336246
NCI-H483	Growth Inhibition Assay				logGI50=-6.56 M	22336246
A549	Growth Inhibition Assay				logGI50=-6.15 M	22336246
DMS273	Growth Inhibition Assay				logGI50=-6.43 M	22336246
DMS114	Growth Inhibition Assay				logGI50=-5.92 M	22336246
LOXIMVI	Growth Inhibition Assay				logGI50=-6.29 M	22336246
OVCAR3	Growth Inhibition Assay				logGI50=-6.71 M	22336246
OVCAR4	Growth Inhibition Assay				logGI50=-5.76 M	22336246
OVCAR5	Growth Inhibition Assay				logGI50=-6.26 M	22336246
OVCAR8	Growth Inhibition Assay				logGI50=-5.73 M	22336246
SKOV3	Growth Inhibition Assay				logGI50=-6.52 M	22336246
RXF631L	Growth Inhibition Assay				logGI50=-6.88 M	22336246
ACHN	Growth Inhibition Assay				logGI50=-6.07 M	22336246
St-4	Growth Inhibition Assay				logGI50=-5.56 M	22336246
MKN1	Growth Inhibition Assay				logGI50=-7.08 M	22336246
MKN7	Growth Inhibition Assay				logGI50=-6.50 M	22336246
MKN28	Growth Inhibition Assay				logGI50=-5.52 M	22336246
MKN45	Growth Inhibition Assay				logGI50=-6.55 M	22336246
MKN74	Growth Inhibition Assay				logGI50=-6.02 M	22336246
DU145	Growth Inhibition Assay				logGI50=-5.85 M	22336246
PC3	Growth Inhibition Assay				logGI50=-6.66 M	22336246
ES5	Growth Inhibition Assay				IC50=50.21 nM	SANGER
HH	Growth Inhibition Assay				IC50=111.08 nM	SANGER
MHH-PREB-1	Growth Inhibition Assay				IC50=114.3 nM	SANGER
NCI-H1770	Growth Inhibition Assay				IC50=123.86 nM	SANGER
HuO9	Growth Inhibition Assay				IC50=206.02 nM	SANGER
HAL-01	Growth Inhibition Assay				IC50=206.73 nM	SANGER
NOS-1	Growth Inhibition Assay				IC50=211.82 nM	SANGER
HGC-27	Growth Inhibition Assay				IC50=212.57 nM	SANGER
NB69	Growth Inhibition Assay				IC50=245.27 nM	SANGER
RS4-11	Growth Inhibition Assay				IC50=261.76 nM	SANGER
DOK	Growth Inhibition Assay				IC50=301.7 nM	SANGER
LB2241-RCC	Growth Inhibition Assay				IC50=303.84 nM	SANGER
NCI-H1623	Growth Inhibition Assay				IC50=304.08 nM	SANGER
YH-13	Growth Inhibition Assay				IC50=304.32 nM	SANGER
BPH-1	Growth Inhibition Assay				IC50=314 nM	SANGER
AN3-CA	Growth Inhibition Assay				IC50=340.37 nM	SANGER
ES7	Growth Inhibition Assay				IC50=341.99 nM	SANGER
MDA-MB-175-VII	Growth Inhibition Assay				IC50=352.92 nM	SANGER
GAMG	Growth Inhibition Assay				IC50=370.85 nM	SANGER
CHL-1	Growth Inhibition Assay				IC50=378.65 nM	SANGER
NB7	Growth Inhibition Assay				IC50=389.83 nM	SANGER
MFE-280	Growth Inhibition Assay				IC50=418.2 nM	SANGER
HL-60	Growth Inhibition Assay				IC50=425.75 nM	SANGER
GCIY	Growth Inhibition Assay				IC50=433.8 nM	SANGER
MDA-MB-361	Growth Inhibition Assay				IC50=439.13 nM	SANGER
LXF-289	Growth Inhibition Assay				IC50=448.27 nM	SANGER
NBsusSR	Growth Inhibition Assay				IC50=488.85 nM	SANGER
KU-19-19	Growth Inhibition Assay				IC50=516.07 nM	SANGER
A204	Growth Inhibition Assay				IC50=522.33 nM	SANGER
LB1047-RCC	Growth Inhibition Assay				IC50=522.93 nM	SANGER
COLO-684	Growth Inhibition Assay				IC50=523.11 nM	SANGER
PA-1	Growth Inhibition Assay				IC50=532.41 nM	SANGER
MG-63	Growth Inhibition Assay				IC50=541.11 nM	SANGER
BHT-101	Growth Inhibition Assay				IC50=544.94 nM	SANGER
NKM-1	Growth Inhibition Assay				IC50=593.09 nM	SANGER
T47D	Growth Inhibition Assay				IC50=597.56 nM	SANGER
MOLT-4	Growth Inhibition Assay				IC50=623.62 nM	SANGER
IGROV-1	Growth Inhibition Assay				IC50=634.31 nM	SANGER
ES4	Growth Inhibition Assay				IC50=639.54 nM	SANGER
HuO-3N1	Growth Inhibition Assay				IC50=642.38 nM	SANGER
NEC8	Growth Inhibition Assay				IC50=653.57 nM	SANGER
HO-1-N-1	Growth Inhibition Assay				IC50=659.17 nM	SANGER
EPCL-272H	Growth Inhibition Assay				IC50=687.21 nM	SANGER
D-263MG	Growth Inhibition Assay				IC50=718.1 nM	SANGER
MV-4-11	Growth Inhibition Assay				IC50=724.31 nM	SANGER
SK-NEP-1	Growth Inhibition Assay				IC50=725.94 nM	SANGER
SW872	Growth Inhibition Assay				IC50=727.89 nM	SANGER
P30-OHK	Growth Inhibition Assay				IC50=730.71 nM	SANGER
OMC-1	Growth Inhibition Assay				IC50=751.09 nM	SANGER
LoVo	Growth Inhibition Assay				IC50=777.9 nM	SANGER
LNCaP-Clone-FGC	Growth Inhibition Assay				IC50=796.34 nM	SANGER
L-363	Growth Inhibition Assay				IC50=798.42 nM	SANGER
ES8	Growth Inhibition Assay				IC50=810.52 nM	SANGER
697	Growth Inhibition Assay				IC50=831.55 nM	SANGER
HSC-3	Growth Inhibition Assay				IC50=839.54 nM	SANGER
H4	Growth Inhibition Assay				IC50=850.85 nM	SANGER
QIMR-WIL	Growth Inhibition Assay				IC50=865.2 nM	SANGER
OAW-42	Growth Inhibition Assay				IC50=872.19 nM	SANGER
MCF7	Growth Inhibition Assay				IC50=898.59 nM	SANGER
SCC-25	Growth Inhibition Assay				IC50=914.19 nM	SANGER
NCI-H1563	Growth Inhibition Assay				IC50=915.99 nM	SANGER
OVCAR-5	Growth Inhibition Assay				IC50=940.17 nM	SANGER
HDLM-2	Growth Inhibition Assay				IC50=949.2 nM	SANGER
NB5	Growth Inhibition Assay				IC50=956.6 nM	SANGER
NCI-H292	Growth Inhibition Assay				IC50=974.32 nM	SANGER
A101D	Growth Inhibition Assay				IC50=990.19 nM	SANGER
NCI-H1648	Growth Inhibition Assay				IC50=998.51 nM	SANGER
EKVX	Growth Inhibition Assay				IC50=1.0129 μM	SANGER
SW1710	Growth Inhibition Assay				IC50=1.04233 μM	SANGER
WM-115	Growth Inhibition Assay				IC50=1.06656 μM	SANGER
CAL-54	Growth Inhibition Assay				IC50=1.07081 μM	SANGER
TGBC24TKB	Growth Inhibition Assay				IC50=1.08045 μM	SANGER
NCI-H520	Growth Inhibition Assay				IC50=1.08967 μM	SANGER
D-423MG	Growth Inhibition Assay				IC50=1.09962 μM	SANGER
BFTC-905	Growth Inhibition Assay				IC50=1.13449 μM	SANGER
HT	Growth Inhibition Assay				IC50=1.13478 μM	SANGER
CTB-1	Growth Inhibition Assay				IC50=1.14293 μM	SANGER
Hs-578-T	Growth Inhibition Assay				IC50=1.19565 μM	SANGER
HuH-7	Growth Inhibition Assay				IC50=1.20949 μM	SANGER
LB996-RCC	Growth Inhibition Assay				IC50=1.22177 μM	SANGER
KYSE-270	Growth Inhibition Assay				IC50=1.29734 μM	SANGER
A4-Fuk	Growth Inhibition Assay				IC50=1.29993 μM	SANGER
A498	Growth Inhibition Assay				IC50=1.30474 μM	SANGER
SK-MEL-1	Growth Inhibition Assay				IC50=1.30679 μM	SANGER
AU565	Growth Inhibition Assay				IC50=1.31863 μM	SANGER
Saos-2	Growth Inhibition Assay				IC50=1.33205 μM	SANGER
A549	Growth Inhibition Assay				IC50=1.3997 μM	SANGER
BFTC-909	Growth Inhibition Assay				IC50=1.43305 μM	SANGER
MDA-MB-415	Growth Inhibition Assay				IC50=1.48692 μM	SANGER
639-V	Growth Inhibition Assay				IC50=1.50245 μM	SANGER
A704	Growth Inhibition Assay				IC50=1.50785 μM	SANGER
PANC-03-27	Growth Inhibition Assay				IC50=1.51408 μM	SANGER
SK-MEL-28	Growth Inhibition Assay				IC50=1.56085 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay				IC50=1.60746 μM	SANGER
HuP-T4	Growth Inhibition Assay				IC50=1.60778 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay				IC50=1.6127 μM	SANGER
EFM-19	Growth Inhibition Assay				IC50=1.6181 μM	SANGER
G-401	Growth Inhibition Assay				IC50=1.62164 μM	SANGER
D-566MG	Growth Inhibition Assay				IC50=1.6253 μM	SANGER
JVM-3	Growth Inhibition Assay				IC50=1.64875 μM	SANGER
TK10	Growth Inhibition Assay				IC50=1.67083 μM	SANGER
BT-20	Growth Inhibition Assay				IC50=1.68902 μM	SANGER
EGI-1	Growth Inhibition Assay				IC50=1.84701 μM	SANGER
EW-16	Growth Inhibition Assay				IC50=1.85182 μM	SANGER
NCI-H2228	Growth Inhibition Assay				IC50=1.85203 μM	SANGER
BB49-HNC	Growth Inhibition Assay				IC50=1.88692 μM	SANGER
G-402	Growth Inhibition Assay				IC50=1.89797 μM	SANGER
NCI-H526	Growth Inhibition Assay				IC50=1.9139 μM	SANGER
ME-180	Growth Inhibition Assay				IC50=1.93477 μM	SANGER
PFSK-1	Growth Inhibition Assay				IC50=1.94458 μM	SANGER
TYK-nu	Growth Inhibition Assay				IC50=1.95823 μM	SANGER
HOS	Growth Inhibition Assay				IC50=1.97948 μM	SANGER
T98G	Growth Inhibition Assay				IC50=1.99006 μM	SANGER
SK-MES-1	Growth Inhibition Assay				IC50=2.01332 μM	SANGER
SNB75	Growth Inhibition Assay				IC50=2.01541 μM	SANGER
LAMA-84	Growth Inhibition Assay				IC50=2.02689 μM	SANGER
CAL-39	Growth Inhibition Assay				IC50=2.0328 μM	SANGER
LOXIMVI	Growth Inhibition Assay				IC50=2.04084 μM	SANGER
NH-12	Growth Inhibition Assay				IC50=2.05424 μM	SANGER
NCI-H1048	Growth Inhibition Assay				IC50=2.1052 μM	SANGER
KS-1	Growth Inhibition Assay				IC50=2.11001 μM	SANGER
NCI-N87	Growth Inhibition Assay				IC50=2.13384 μM	SANGER
CHP-212	Growth Inhibition Assay				IC50=2.18442 μM	SANGER
HCC1419	Growth Inhibition Assay				IC50=2.21115 μM	SANGER
ES1	Growth Inhibition Assay				IC50=2.21326 μM	SANGER
NCI-H2030	Growth Inhibition Assay				IC50=2.24123 μM	SANGER
EW-22	Growth Inhibition Assay				IC50=2.25067 μM	SANGER
A431	Growth Inhibition Assay				IC50=2.27354 μM	SANGER
SF126	Growth Inhibition Assay				IC50=2.30625 μM	SANGER
SF295	Growth Inhibition Assay				IC50=2.31524 μM	SANGER
D-502MG	Growth Inhibition Assay				IC50=2.32461 μM	SANGER
HCC2157	Growth Inhibition Assay				IC50=2.32927 μM	SANGER
D-283MED	Growth Inhibition Assay				IC50=2.35926 μM	SANGER
SNU-423	Growth Inhibition Assay				IC50=2.40171 μM	SANGER
SK-LU-1	Growth Inhibition Assay				IC50=2.44586 μM	SANGER
22RV1	Growth Inhibition Assay				IC50=2.45617 μM	SANGER
SW1088	Growth Inhibition Assay				IC50=2.49213 μM	SANGER
HT-3	Growth Inhibition Assay				IC50=2.49259 μM	SANGER
NCI-H1666	Growth Inhibition Assay				IC50=2.51104 μM	SANGER
EM-2	Growth Inhibition Assay				IC50=2.51169 μM	SANGER
SNU-449	Growth Inhibition Assay				IC50=2.57014 μM	SANGER
786-0	Growth Inhibition Assay				IC50=2.59238 μM	SANGER
SKG-IIIa	Growth Inhibition Assay				IC50=2.65939 μM	SANGER
MEL-HO	Growth Inhibition Assay				IC50=2.67634 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay				IC50=2.69267 μM	SANGER
MKN7	Growth Inhibition Assay				IC50=2.70754 μM	SANGER
5637	Growth Inhibition Assay				IC50=2.71035 μM	SANGER
HOP-92	Growth Inhibition Assay				IC50=2.74717 μM	SANGER
MDA-MB-157	Growth Inhibition Assay				IC50=2.82023 μM	SANGER
NB12	Growth Inhibition Assay				IC50=2.84914 μM	SANGER
DMS-273	Growth Inhibition Assay				IC50=2.8647 μM	SANGER
HCC70	Growth Inhibition Assay				IC50=2.86589 μM	SANGER
YKG-1	Growth Inhibition Assay				IC50=3.03787 μM	SANGER
NCI-H28	Growth Inhibition Assay				IC50=3.05291 μM	SANGER
HN	Growth Inhibition Assay				IC50=3.06636 μM	SANGER
HT-1080	Growth Inhibition Assay				IC50=3.08606 μM	SANGER
HPAF-II	Growth Inhibition Assay				IC50=3.10068 μM	SANGER
U-2-OS	Growth Inhibition Assay				IC50=3.13782 μM	SANGER
SNU-387	Growth Inhibition Assay				IC50=3.16364 μM	SANGER
Becker	Growth Inhibition Assay				IC50=3.16808 μM	SANGER
BHY	Growth Inhibition Assay				IC50=3.25571 μM	SANGER
HTC-C3	Growth Inhibition Assay				IC50=3.29352 μM	SANGER
M14	Growth Inhibition Assay				IC50=3.30663 μM	SANGER
COR-L23	Growth Inhibition Assay				IC50=3.37279 μM	SANGER
C32	Growth Inhibition Assay				IC50=3.41508 μM	SANGER
Mewo	Growth Inhibition Assay				IC50=3.42182 μM	SANGER
TE-8	Growth Inhibition Assay				IC50=3.48259 μM	SANGER
RPMI-2650	Growth Inhibition Assay				IC50=3.60637 μM	SANGER
AGS	Growth Inhibition Assay				IC50=3.62464 μM	SANGER
MZ2-MEL	Growth Inhibition Assay				IC50=3.66138 μM	SANGER
Calu-3	Growth Inhibition Assay				IC50=3.71287 μM	SANGER
SJSA-1	Growth Inhibition Assay				IC50=3.71315 μM	SANGER
SW962	Growth Inhibition Assay				IC50=3.72636 μM	SANGER
PC-14	Growth Inhibition Assay				IC50=3.73222 μM	SANGER
SW1573	Growth Inhibition Assay				IC50=3.75348 μM	SANGER
769-P	Growth Inhibition Assay				IC50=3.82743 μM	SANGER
KNS-62	Growth Inhibition Assay				IC50=3.92338 μM	SANGER
NCI-H747	Growth Inhibition Assay				IC50=4.05638 μM	SANGER
LN-405	Growth Inhibition Assay				IC50=4.15728 μM	SANGER
OVCAR-8	Growth Inhibition Assay				IC50=4.22543 μM	SANGER
DMS-114	Growth Inhibition Assay				IC50=4.23891 μM	SANGER
NCI-H2126	Growth Inhibition Assay				IC50=4.24558 μM	SANGER
TCCSUP	Growth Inhibition Assay				IC50=4.24788 μM	SANGER
SK-N-FI	Growth Inhibition Assay				IC50=4.25332 μM	SANGER
HCE-4	Growth Inhibition Assay				IC50=4.27197 μM	SANGER
DK-MG	Growth Inhibition Assay				IC50=4.3039 μM	SANGER
RO82-W-1	Growth Inhibition Assay				IC50=4.32584 μM	SANGER
A2780	Growth Inhibition Assay				IC50=4.36682 μM	SANGER
ETK-1	Growth Inhibition Assay				IC50=4.37052 μM	SANGER
FADU	Growth Inhibition Assay				IC50=4.37467 μM	SANGER
CAL-12T	Growth Inhibition Assay				IC50=4.41413 μM	SANGER
647-V	Growth Inhibition Assay				IC50=4.44022 μM	SANGER
TGBC1TKB	Growth Inhibition Assay				IC50=4.45113 μM	SANGER
LU-99A	Growth Inhibition Assay				IC50=4.4606 μM	SANGER
CAL-33	Growth Inhibition Assay				IC50=4.52456 μM	SANGER
LU-134-A	Growth Inhibition Assay				IC50=4.52745 μM	SANGER
NCI-H1355	Growth Inhibition Assay				IC50=4.55146 μM	SANGER
RPMI-7951	Growth Inhibition Assay				IC50=4.57002 μM	SANGER
TE-1	Growth Inhibition Assay				IC50=4.66143 μM	SANGER
OE33	Growth Inhibition Assay				IC50=4.70511 μM	SANGER
CAL-51	Growth Inhibition Assay				IC50=4.71082 μM	SANGER
SW1783	Growth Inhibition Assay				IC50=4.75308 μM	SANGER
BT-474	Growth Inhibition Assay				IC50=4.76384 μM	SANGER
KYSE-520	Growth Inhibition Assay				IC50=4.87392 μM	SANGER
8-MG-BA	Growth Inhibition Assay				IC50=4.88557 μM	SANGER
IA-LM	Growth Inhibition Assay				IC50=4.99435 μM	SANGER
SW954	Growth Inhibition Assay				IC50=4.99443 μM	SANGER
RPMI-8226	Growth Inhibition Assay				IC50=5.05461 μM	SANGER
MKN1	Growth Inhibition Assay				IC50=5.07927 μM	SANGER
A375	Growth Inhibition Assay				IC50=5.09256 μM	SANGER
8305C	Growth Inhibition Assay				IC50=5.09887 μM	SANGER
CAL-62	Growth Inhibition Assay				IC50=5.18259 μM	SANGER
NB10	Growth Inhibition Assay				IC50=5.22744 μM	SANGER
OC-314	Growth Inhibition Assay				IC50=5.37444 μM	SANGER
PSN1	Growth Inhibition Assay				IC50=5.38286 μM	SANGER
GR-ST	Growth Inhibition Assay				IC50=5.38322 μM	SANGER
P12-ICHIKAWA	Growth Inhibition Assay				IC50=5.401 μM	SANGER
NCI-H1092	Growth Inhibition Assay				IC50=5.41148 μM	SANGER
SCC-4	Growth Inhibition Assay				IC50=5.41355 μM	SANGER
TE-6	Growth Inhibition Assay				IC50=5.41816 μM	SANGER
DOHH-2	Growth Inhibition Assay				IC50=5.42248 μM	SANGER
SW684	Growth Inhibition Assay				IC50=5.66385 μM	SANGER
CP50-MEL-B	Growth Inhibition Assay				IC50=5.68684 μM	SANGER
UM-UC-3	Growth Inhibition Assay				IC50=5.72231 μM	SANGER
LC-2-ad	Growth Inhibition Assay				IC50=5.78251 μM	SANGER
PC-3	Growth Inhibition Assay				IC50=5.91615 μM	SANGER
CAN	Growth Inhibition Assay				IC50=5.9282 μM	SANGER
ESS-1	Growth Inhibition Assay				IC50=5.97869 μM	SANGER
ATN-1	Growth Inhibition Assay				IC50=6.05568 μM	SANGER
BxPC-3	Growth Inhibition Assay				IC50=6.08219 μM	SANGER
KYSE-150	Growth Inhibition Assay				IC50=6.12476 μM	SANGER
RPMI-8866	Growth Inhibition Assay				IC50=6.19163 μM	SANGER
SW780	Growth Inhibition Assay				IC50=6.2042 μM	SANGER
A388	Growth Inhibition Assay				IC50=6.23115 μM	SANGER
NCI-H1437	Growth Inhibition Assay				IC50=6.24073 μM	SANGER
NCI-H1755	Growth Inhibition Assay				IC50=6.36612 μM	SANGER
LS-123	Growth Inhibition Assay				IC50=6.40521 μM	SANGER
CaR-1	Growth Inhibition Assay				IC50=6.46373 μM	SANGER
RT-112	Growth Inhibition Assay				IC50=6.60338 μM	SANGER
CGT	Growth Inhibition Assay				IC50=6.73681 μM	SANGER
SW626	Growth Inhibition Assay				IC50=6.73946 μM	SANGER
AsPC-1	Growth Inhibition Assay				IC50=6.74507 μM	SANGER
SBC-5	Growth Inhibition Assay				IC50=6.97297 μM	SANGER
SF539	Growth Inhibition Assay				IC50=6.99333 μM	SANGER
TI-73	Growth Inhibition Assay				IC50=7.06285 μM	SANGER
MHH-ES-1	Growth Inhibition Assay				IC50=7.07762 μM	SANGER
KYSE-510	Growth Inhibition Assay				IC50=7.08432 μM	SANGER
EW-1	Growth Inhibition Assay				IC50=7.36996 μM	SANGER
SK-OV-3	Growth Inhibition Assay				IC50=7.39432 μM	SANGER
MC-IXC	Growth Inhibition Assay				IC50=7.41972 μM	SANGER
HSC-2	Growth Inhibition Assay				IC50=7.42705 μM	SANGER
NCI-H2342	Growth Inhibition Assay				IC50=7.5149 μM	SANGER
NCI-H1792	Growth Inhibition Assay				IC50=7.51711 μM	SANGER
HT-1376	Growth Inhibition Assay				IC50=7.87778 μM	SANGER
EW-13	Growth Inhibition Assay				IC50=7.89977 μM	SANGER
no-11	Growth Inhibition Assay				IC50=7.90174 μM	SANGER
Daoy	Growth Inhibition Assay				IC50=7.94321 μM	SANGER
COLO-800	Growth Inhibition Assay				IC50=8.04162 μM	SANGER
GB-1	Growth Inhibition Assay				IC50=8.06565 μM	SANGER
SJRH30	Growth Inhibition Assay				IC50=8.15878 μM	SANGER
NCI-H2291	Growth Inhibition Assay				IC50=8.29187 μM	SANGER
J82	Growth Inhibition Assay				IC50=8.29491 μM	SANGER
NCI-H596	Growth Inhibition Assay				IC50=8.31453 μM	SANGER
RERF-LC-MS	Growth Inhibition Assay				IC50=8.34856 μM	SANGER
RH-18	Growth Inhibition Assay				IC50=8.35046 μM	SANGER
SW48	Growth Inhibition Assay				IC50=8.59453 μM	SANGER
RD	Growth Inhibition Assay				IC50=8.59391 μM	SANGER
MS-1	Growth Inhibition Assay				IC50=8.61387 μM	SANGER
ES6	Growth Inhibition Assay				IC50=8.73119 μM	SANGER
TE-12	Growth Inhibition Assay				IC50=8.77505 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay				IC50=8.91217 μM	SANGER
KINGS-1	Growth Inhibition Assay				IC50=8.92938 μM	SANGER
HLE	Growth Inhibition Assay				IC50=8.93785 μM	SANGER
MHH-NB-11	Growth Inhibition Assay				IC50=9.01839 μM	SANGER
U-87-MG	Growth Inhibition Assay				IC50=9.24321 μM	SANGER
MN-60	Growth Inhibition Assay				IC50=9.24542 μM	SANGER
SAS	Growth Inhibition Assay				IC50=9.25581 μM	SANGER
NCI-H446	Growth Inhibition Assay				IC50=9.361 μM	SANGER
C-33-A	Growth Inhibition Assay				IC50=9.43988 μM	SANGER
RXF393	Growth Inhibition Assay				IC50=9.47002 μM	SANGER
CGTH-W-1	Growth Inhibition Assay				IC50=9.49384 μM	SANGER
RCM-1	Growth Inhibition Assay				IC50=9.63801 μM	SANGER
SN12C	Growth Inhibition Assay				IC50=9.65338 μM	SANGER
KLE	Growth Inhibition Assay				IC50=9.70009 μM	SANGER
EFO-21	Growth Inhibition Assay				IC50=9.77382 μM	SANGER
KYSE-70	Growth Inhibition Assay				IC50=9.88011 μM	SANGER
D-247MG	Growth Inhibition Assay				IC50=10.0568 μM	SANGER
MPP-89	Growth Inhibition Assay				IC50=10.0946 μM	SANGER
RVH-421	Growth Inhibition Assay				IC50=10.1505 μM	SANGER
NCI-H460	Growth Inhibition Assay				IC50=10.2806 μM	SANGER
NOMO-1	Growth Inhibition Assay				IC50=10.3532 μM	SANGER
DEL	Growth Inhibition Assay				IC50=10.3794 μM	SANGER
HT55	Growth Inhibition Assay				IC50=10.6205 μM	SANGER
MC116	Growth Inhibition Assay				IC50=10.6655 μM	SANGER
BB30-HNC	Growth Inhibition Assay				IC50=10.669 μM	SANGER
DJM-1	Growth Inhibition Assay				IC50=10.6949 μM	SANGER
ZR-75-30	Growth Inhibition Assay				IC50=10.9441 μM	SANGER
U-118-MG	Growth Inhibition Assay				IC50=10.9896 μM	SANGER
MSTO-211H	Growth Inhibition Assay				IC50=11.0716 μM	SANGER
SW837	Growth Inhibition Assay				IC50=11.0949 μM	SANGER
HuCCT1	Growth Inhibition Assay				IC50=11.1281 μM	SANGER
RCC10RGB	Growth Inhibition Assay				IC50=11.135 μM	SANGER
NMC-G1	Growth Inhibition Assay				IC50=11.1493 μM	SANGER
NCI-H650	Growth Inhibition Assay				IC50=11.3794 μM	SANGER
HEC-1	Growth Inhibition Assay				IC50=11.4328 μM	SANGER
DU-4475	Growth Inhibition Assay				IC50=11.7393 μM	SANGER
DSH1	Growth Inhibition Assay				IC50=11.7606 μM	SANGER
HCC1569	Growth Inhibition Assay				IC50=11.7678 μM	SANGER
HCC1187	Growth Inhibition Assay				IC50=11.8588 μM	SANGER
EW-11	Growth Inhibition Assay				IC50=11.9474 μM	SANGER
LB2518-MEL	Growth Inhibition Assay				IC50=12.059 μM	SANGER
KALS-1	Growth Inhibition Assay				IC50=12.8553 μM	SANGER
8505C	Growth Inhibition Assay				IC50=12.885 μM	SANGER
SK-N-DZ	Growth Inhibition Assay				IC50=13.0453 μM	SANGER
CHP-134	Growth Inhibition Assay				IC50=13.1158 μM	SANGER
HCE-T	Growth Inhibition Assay				IC50=13.2364 μM	SANGER
LB-831-BLC	Growth Inhibition Assay				IC50=13.6246 μM	SANGER
OVCAR-4	Growth Inhibition Assay				IC50=13.6524 μM	SANGER
SW756	Growth Inhibition Assay				IC50=13.7246 μM	SANGER
OCUB-M	Growth Inhibition Assay				IC50=13.8156 μM	SANGER
SW982	Growth Inhibition Assay				IC50=13.8276 μM	SANGER
DB	Growth Inhibition Assay				IC50=13.8384 μM	SANGER
H-EMC-SS	Growth Inhibition Assay				IC50=13.9139 μM	SANGER
VMRC-RCZ	Growth Inhibition Assay				IC50=14.0015 μM	SANGER
CAKI-1	Growth Inhibition Assay				IC50=14.0132 μM	SANGER
GI-1	Growth Inhibition Assay				IC50=14.0658 μM	SANGER
Ca9-22	Growth Inhibition Assay				IC50=14.6054 μM	SANGER
TE-5	Growth Inhibition Assay				IC50=14.7208 μM	SANGER
EFO-27	Growth Inhibition Assay				IC50=14.7622 μM	SANGER
CAL-72	Growth Inhibition Assay				IC50=14.7783 μM	SANGER
GP5d	Growth Inhibition Assay				IC50=15.0474 μM	SANGER
CAS-1	Growth Inhibition Assay				IC50=15.066 μM	SANGER
A2058	Growth Inhibition Assay				IC50=15.5638 μM	SANGER
PANC-08-13	Growth Inhibition Assay				IC50=15.6859 μM	SANGER
Detroit562	Growth Inhibition Assay				IC50=15.9139 μM	SANGER
PANC-10-05	Growth Inhibition Assay				IC50=16.0821 μM	SANGER
KOSC-2	Growth Inhibition Assay				IC50=16.1125 μM	SANGER
GT3TKB	Growth Inhibition Assay				IC50=16.1981 μM	SANGER
KM-H2	Growth Inhibition Assay				IC50=16.3646 μM	SANGER
LB771-HNC	Growth Inhibition Assay				IC50=16.4422 μM	SANGER
SF268	Growth Inhibition Assay				IC50=16.452 μM	SANGER
OE19	Growth Inhibition Assay				IC50=16.524 μM	SANGER
MLMA	Growth Inhibition Assay				IC50=16.5571 μM	SANGER
MDA-MB-231	Growth Inhibition Assay				IC50=16.7136 μM	SANGER
TGW	Growth Inhibition Assay				IC50=16.8102 μM	SANGER
MDA-MB-453	Growth Inhibition Assay				IC50=17.0003 μM	SANGER
SNU-C2B	Growth Inhibition Assay				IC50=17.0237 μM	SANGER
A427	Growth Inhibition Assay				IC50=17.2334 μM	SANGER
SK-MEL-2	Growth Inhibition Assay				IC50=17.3213 μM	SANGER
KURAMOCHI	Growth Inhibition Assay				IC50=17.3897 μM	SANGER
IST-MEL1	Growth Inhibition Assay				IC50=17.9182 μM	SANGER
NCI-H1793	Growth Inhibition Assay				IC50=18.1581 μM	SANGER
HCC1395	Growth Inhibition Assay				IC50=18.5611 μM	SANGER
NUGC-3	Growth Inhibition Assay				IC50=18.6584 μM	SANGER
BB65-RCC	Growth Inhibition Assay				IC50=18.669 μM	SANGER
RMG-I	Growth Inhibition Assay				IC50=18.7382 μM	SANGER
LS-513	Growth Inhibition Assay				IC50=18.9228 μM	SANGER
MFM-223	Growth Inhibition Assay				IC50=19.0716 μM	SANGER
NCI-H727	Growth Inhibition Assay				IC50=19.3295 μM	SANGER
KP-4	Growth Inhibition Assay				IC50=19.8531 μM	SANGER
NB13	Growth Inhibition Assay				IC50=19.8839 μM	SANGER
UACC-893	Growth Inhibition Assay				IC50=19.9757 μM	SANGER
HT-1197	Growth Inhibition Assay				IC50=20.2958 μM	SANGER
NCI-H2029	Growth Inhibition Assay				IC50=20.3266 μM	SANGER
GI-ME-N	Growth Inhibition Assay				IC50=20.3373 μM	SANGER
OVCAR-3	Growth Inhibition Assay				IC50=20.5822 μM	SANGER
HD-MY-Z	Growth Inhibition Assay				IC50=21.3696 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay				IC50=21.6722 μM	SANGER
SCH	Growth Inhibition Assay				IC50=22.496 μM	SANGER
KARPAS-299	Growth Inhibition Assay				IC50=23.3887 μM	SANGER
NCI-H1650	Growth Inhibition Assay				IC50=23.9241 μM	SANGER
ACHN	Growth Inhibition Assay				IC50=24.4656 μM	SANGER
M059J	Growth Inhibition Assay				IC50=24.5634 μM	SANGER
AM-38	Growth Inhibition Assay				IC50=25.481 μM	SANGER
KG-1	Growth Inhibition Assay				IC50=25.5494 μM	SANGER
COLO-824	Growth Inhibition Assay				IC50=25.5599 μM	SANGER
NCI-H1155	Growth Inhibition Assay				IC50=25.5847 μM	SANGER
NCI-H441	Growth Inhibition Assay				IC50=25.7465 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay				IC50=26.3027 μM	SANGER
JEG-3	Growth Inhibition Assay				IC50=26.6805 μM	SANGER
RKO	Growth Inhibition Assay				IC50=26.7632 μM	SANGER
CAL-85-1	Growth Inhibition Assay				IC50=27.2118 μM	SANGER
CAL-120	Growth Inhibition Assay				IC50=27.6914 μM	SANGER
NCI-H2452	Growth Inhibition Assay				IC50=27.7716 μM	SANGER
NCI-H1395	Growth Inhibition Assay				IC50=27.7833 μM	SANGER
KYSE-450	Growth Inhibition Assay				IC50=27.9862 μM	SANGER
S-117	Growth Inhibition Assay				IC50=29.3857 μM	SANGER
SW13	Growth Inhibition Assay				IC50=29.8519 μM	SANGER
ES3	Growth Inhibition Assay				IC50=30.3733 μM	SANGER
HCT-116	Growth Inhibition Assay				IC50=30.5554 μM	SANGER
NCI-H1693	Growth Inhibition Assay				IC50=30.5942 μM	SANGER
VM-CUB-1	Growth Inhibition Assay				IC50=30.6413 μM	SANGER
NCI-H2170	Growth Inhibition Assay				IC50=31.5784 μM	SANGER
ALL-PO	Growth Inhibition Assay				IC50=31.8428 μM	SANGER
NCI-H661	Growth Inhibition Assay				IC50=32.0623 μM	SANGER
NCI-H2347	Growth Inhibition Assay				IC50=32.4837 μM	SANGER
FTC-133	Growth Inhibition Assay				IC50=32.706 μM	SANGER
COLO-829	Growth Inhibition Assay				IC50=33.3467 μM	SANGER
GOTO	Growth Inhibition Assay				IC50=33.5258 μM	SANGER
YAPC	Growth Inhibition Assay				IC50=33.8159 μM	SANGER
LCLC-103H	Growth Inhibition Assay				IC50=34.1624 μM	SANGER
SiHa	Growth Inhibition Assay				IC50=34.3817 μM	SANGER
LK-2	Growth Inhibition Assay				IC50=34.5708 μM	SANGER
KP-N-YS	Growth Inhibition Assay				IC50=34.7202 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay				IC50=35.179 μM	SANGER
KNS-81-FD	Growth Inhibition Assay				IC50=35.663 μM	SANGER
SCC-9	Growth Inhibition Assay				IC50=36.7146 μM	SANGER
SH-4	Growth Inhibition Assay				IC50=36.73 μM	SANGER
HCC-1954	Growth Inhibition Assay				IC50=37.2729 μM	SANGER
BALL-1	Growth Inhibition Assay				IC50=37.5316 μM	SANGER
BE-13	Growth Inhibition Assay				IC50=37.7018 μM	SANGER
COLO-678	Growth Inhibition Assay				IC50=37.9437 μM	SANGER
SK-MEL-3	Growth Inhibition Assay				IC50=38.2397 μM	SANGER
OAW-28	Growth Inhibition Assay				IC50=38.639 μM	SANGER
CAMA-1	Growth Inhibition Assay				IC50=38.9691 μM	SANGER
C2BBe1	Growth Inhibition Assay				IC50=39.818 μM	SANGER
A3-KAW	Growth Inhibition Assay				IC50=40.3661 μM	SANGER
SK-MEL-24	Growth Inhibition Assay				IC50=40.5931 μM	SANGER
KYSE-140	Growth Inhibition Assay				IC50=40.7165 μM	SANGER
MOLT-16	Growth Inhibition Assay				IC50=41.1536 μM	SANGER
CFPAC-1	Growth Inhibition Assay				IC50=42.5211 μM	SANGER
NB14	Growth Inhibition Assay				IC50=42.7027 μM	SANGER
COLO-792	Growth Inhibition Assay				IC50=42.8961 μM	SANGER
RH-1	Growth Inhibition Assay				IC50=43.4836 μM	SANGER
NCI-H522	Growth Inhibition Assay				IC50=44.3568 μM	SANGER
Ca-Ski	Growth Inhibition Assay				IC50=44.8114 μM	SANGER
KGN	Growth Inhibition Assay				IC50=48.3063 μM	SANGER
UACC-62	Growth Inhibition Assay				IC50=48.4072 μM	SANGER
NCI-H358	Growth Inhibition Assay				IC50=49.3018 μM	SANGER
LS-411N	Growth Inhibition Assay				IC50=49.3118 μM	SANGER
IST-MES1	Growth Inhibition Assay				IC50=49.5625 μM	SANGER
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (194.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	513.64	Formula	C₂₃H₂₇N₇O₃S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	957054-30-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RG7321			Smiles	CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6

Mechanism of Action

Targets/IC₅₀/Ki	p110α (Cell-free assay) 3 nM p110δ (Cell-free assay) 3 nM p110β (Cell-free assay) 33 nM p110γ (Cell-free assay) 75 nM mTOR (Cell-free assay) 0.58 μM(Ki app)
In vitro	Pictilisib (GDC-0941) is equipotent against PI3Kα and PI3Kδ as well as PI3Kα mutants E545-K and H1047-R, displaying modest levels of selectivity against PI3Kβ (10-fold) and PI3Kγ (25-fold), and greater levels of selectivity against members of PI3K class II, III, and IV, including C2β, Vps34, DNA-PK, and mTOR. It potently inhibits the phosphorylation of Akt in U87MG, PC3, and MDA-MB-361 cells with IC50 of 46 nM, 37 nM, and 28 nM, respectively. This compound inhibits the proliferation of U87MG, A2780, PC3, and MDA-MB-361 cells with IC50 of 0.95 μM, 0.14 μM, 0.28 μM, and 0.72 μM, respectively. It inhibits proliferation of HER2-amplified cells that harbor PIK3CA mutations with IC50 of <500 nM, and effectively inhibits both proliferation and viability of HER2-amplified breast cancer cells. It significantly inhibits the growth of HCT116, DLD1 and HT29 cells with GI50 of 1081 nM, 1070 nM and 157 nM, respectively. It also inhibits tumor cell proliferation, induces apoptosis and suppresses centroblast population.
Kinase Assay	Scintillation proximity assay
Kinase Assay	Recombinant human PI3Kα, PI3Kβ, and PI3Kδ are coexpressed in a Sf9 baculovirus system with the p85α regulatory subunit and purified as GST-fusion proteins using affinity chromatography. Recombinant human PI3Kγ is expressed as monomeric GST-fusions and purified similarly. Pictilisib (GDC-0941) is dissolved in DMSO and added to 20 mM Tris-HCl (pH 7.5) containing 200 μg yttrium silicate (Ysi) polylysine SPA beads, 4 mM MgCl₂, 1 mM dithiothreitol (DTT), 1 μM ATP, 0.125 μCi [γ-³³P]-ATP, and 4% (v/v) DMSO in a total volume of 50 μL. The recombinant GST-fusion of PI3Kα (5 ng), PI3Kβ (5 ng), PI3Kδ (5 ng), or PI3Kγ (5 ng) is added to the assay mixture to initiate the kinase reaction. After incubation for 1 hour at room temperature, the kinase reaction is terminated with 150 μL PBS. The mixture is then centrifuged for 2 minutes at 2000 rpm and read using a Wallac Microbeta counter. The reported IC50 values are calculated using a sigmoidal, dose-response curve fit in MDL Assay Explorer.
In vivo	Pictilisib (GDC-0941) shows limited microsomal metabolism, resulting in 78% oral bioavailability . Administration of this compound at 75 mg/kg/day displays significant inhibitory effect against established human U87MG glioblastoma xenografts in female NCr athymic mice, with tumor growth inhibition of 83%. Oral administration of it at 150 mg/kg/day inhibits the growth of HER2-amplified, MDA-MB-361.1 xenografts in mice, and significantly delays the tumor progression, in association with potent induced apoptosis in tumors. Treatment with it (75 mg/kg/day) for 2 weeks induces ~40% reduction in tumor volume of spontaneous B-cell follicular lymphomas developed in PTEN+/-LKB1+/hypo mice, accompanied by ablation of phosphorylation of Akt, S6K and SGK (serum and glucocorticoid protein kinase) protein kinases.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18754654/ [2] https://pubmed.ncbi.nlm.nih.gov/19411071/ [3] https://pubmed.ncbi.nlm.nih.gov/22415236/ [4] https://pubmed.ncbi.nlm.nih.gov/21407213/ [5] https://pubmed.ncbi.nlm.nih.gov/19584227/

Applications

Methods	Biomarkers	PMID
Western blot	p-AKT / AKT / p-FoxO3a / FoxO3a / PUMA p-S6RP / S6RP p-4EBP1 / 4EBP1 p-LRP6 / LRP6 p-PAK / PAK1 / p-CRAF / RAF / p-MEK / MEK / p-ERK / ERK	29137323
Immunofluorescence	p65 beta-catenin	30042442
Growth inhibition assay	Cell viability	27117832

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02092831	Completed	Healthy Volunteer	Genentech Inc.	April 2014	Phase 1
NCT01740336	Completed	Breast Cancer	Genentech Inc.	February 6 2013	Phase 2
NCT01474668	Completed	Healthy Volunteer	Genentech Inc.	October 2011	Phase 1
NCT01240226	Completed	Healthy Volunteer	Genentech Inc.	November 2010	Phase 1

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