Nilotinib

Synonyms: AMN-107

Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.

Nilotinib Chemical Structure

Nilotinib Chemical Structure

CAS No. 641571-10-0

Purity & Quality Control

Nilotinib Related Products

Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell Growth Inhibition Assay IC50=0.000144 μM SANGER
KU812 Growth Inhibition Assay IC50=0.00248 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.0041 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.0049 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.00828 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.01089 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=0.02413 μM SANGER
NB7 Growth Inhibition Assay IC50=0.13439 μM SANGER
BHT-101 Growth Inhibition Assay IC50=0.64263 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.6487 μM SANGER
HMV-II Growth Inhibition Assay IC50=0.74874 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.9015 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=1.02228 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=1.1887 μM SANGER
BE-13 Growth Inhibition Assay IC50=1.27416 μM SANGER
ACN Growth Inhibition Assay IC50=1.55077 μM SANGER
A204 Growth Inhibition Assay IC50=1.57205 μM SANGER
HOP-62 Growth Inhibition Assay IC50=1.82077 μM SANGER
H9 Growth Inhibition Assay IC50=2.73793 μM SANGER
HCC1806 Growth Inhibition Assay IC50=2.74327 μM SANGER
NOS-1 Growth Inhibition Assay IC50=2.87102 μM SANGER
RS4-11 Growth Inhibition Assay IC50=2.90623 μM SANGER
JAR Growth Inhibition Assay IC50=2.92084 μM SANGER
T98G Growth Inhibition Assay IC50=3.01313 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=3.40092 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=3.43029 μM SANGER
L-363 Growth Inhibition Assay IC50=3.61107 μM SANGER
SW982 Growth Inhibition Assay IC50=3.64169 μM SANGER
HT-1080 Growth Inhibition Assay IC50=3.91775 μM SANGER
G-402 Growth Inhibition Assay IC50=4.31203 μM SANGER
HOS Growth Inhibition Assay IC50=4.80282 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=4.83191 μM SANGER
HAL-01 Growth Inhibition Assay IC50=4.88242 μM SANGER
SBC-1 Growth Inhibition Assay IC50=4.90907 μM SANGER
CTV-1 Growth Inhibition Assay IC50=5.48938 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=5.77471 μM SANGER
RVH-421 Growth Inhibition Assay IC50=5.77536 μM SANGER
K-562 Growth Inhibition Assay IC50=5.9036 μM SANGER
CAL-33 Growth Inhibition Assay IC50=6.31359 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=6.33699 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=6.47191 μM SANGER
NY Growth Inhibition Assay IC50=6.53599 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=6.66931 μM SANGER
HuO9 Growth Inhibition Assay IC50=6.73964 μM SANGER
MS-1 Growth Inhibition Assay IC50=7.11953 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=7.28287 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=7.40149 μM SANGER
D-566MG Growth Inhibition Assay IC50=7.47155 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=7.63392 μM SANGER
COLO-679 Growth Inhibition Assay IC50=7.98671 μM SANGER
EW-13 Growth Inhibition Assay IC50=8.32054 μM SANGER
A388 Growth Inhibition Assay IC50=8.38481 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=8.43956 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=8.53582 μM SANGER
COLO-668 Growth Inhibition Assay IC50=8.59491 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=8.62353 μM SANGER
D-423MG Growth Inhibition Assay IC50=8.83756 μM SANGER
CTB-1 Growth Inhibition Assay IC50=8.87128 μM SANGER
BCPAP Growth Inhibition Assay IC50=9.02562 μM SANGER
GCT Growth Inhibition Assay IC50=9.09831 μM SANGER
ACHN Growth Inhibition Assay IC50=9.23632 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=9.33482 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=9.76497 μM SANGER
MLMA Growth Inhibition Assay IC50=10.0132 μM SANGER
HEC-1 Growth Inhibition Assay IC50=10.2804 μM SANGER
HL-60 Growth Inhibition Assay IC50=10.6853 μM SANGER
A101D Growth Inhibition Assay IC50=10.8923 μM SANGER
A2058 Growth Inhibition Assay IC50=10.9245 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=11.0635 μM SANGER
697 Growth Inhibition Assay IC50=11.2101 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=11.7731 μM SANGER
DSH1 Growth Inhibition Assay IC50=11.7953 μM SANGER
HLE Growth Inhibition Assay IC50=11.8839 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=12.6801 μM SANGER
EW-3 Growth Inhibition Assay IC50=12.9307 μM SANGER
AGS Growth Inhibition Assay IC50=13.0351 μM SANGER
ES5 Growth Inhibition Assay IC50=13.0512 μM SANGER
DB Growth Inhibition Assay IC50=13.3256 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=13.4102 μM SANGER
A427 Growth Inhibition Assay IC50=13.4972 μM SANGER
MN-60 Growth Inhibition Assay IC50=13.5843 μM SANGER
HCC2218 Growth Inhibition Assay IC50=13.5856 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=13.8137 μM SANGER
GI-1 Growth Inhibition Assay IC50=14.1184 μM SANGER
JVM-3 Growth Inhibition Assay IC50=14.2656 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=14.2727 μM SANGER
TE-12 Growth Inhibition Assay IC50=14.6046 μM SANGER
WM-115 Growth Inhibition Assay IC50=15.5683 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=16.0241 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=16.3802 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=16.6203 μM SANGER
UACC-257 Growth Inhibition Assay IC50=17.0582 μM SANGER
RKO Growth Inhibition Assay IC50=17.6433 μM SANGER
HT-29 Growth Inhibition Assay IC50=17.7889 μM SANGER
ES7 Growth Inhibition Assay IC50=18.1122 μM SANGER
DEL Growth Inhibition Assay IC50=18.3172 μM SANGER
BT-549 Growth Inhibition Assay IC50=18.4092 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=18.5723 μM SANGER
HCE-T Growth Inhibition Assay IC50=18.8341 μM SANGER
LU-139 Growth Inhibition Assay IC50=19.0458 μM SANGER
ECC10 Growth Inhibition Assay IC50=19.2475 μM SANGER
769-P Growth Inhibition Assay IC50=19.6335 μM SANGER
BALL-1 Growth Inhibition Assay IC50=19.6775 μM SANGER
LXF-289 Growth Inhibition Assay IC50=19.8979 μM SANGER
TYK-nu Growth Inhibition Assay IC50=19.9315 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=19.9378 μM SANGER
EW-18 Growth Inhibition Assay IC50=20.3802 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=20.7047 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=20.7586 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=21.0852 μM SANGER
MFE-280 Growth Inhibition Assay IC50=21.5679 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=21.8408 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=22.0478 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=22.4299 μM SANGER
TE-5 Growth Inhibition Assay IC50=22.4965 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=22.4971 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=23.2843 μM SANGER
RH-1 Growth Inhibition Assay IC50=23.5357 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=23.8472 μM SANGER
Mo-T Growth Inhibition Assay IC50=23.9 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=24.2362 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=24.6767 μM SANGER
C32 Growth Inhibition Assay IC50=24.9576 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=25.3577 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=25.3943 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=25.4577 μM SANGER
HT-1197 Growth Inhibition Assay IC50=25.5319 μM SANGER
A172 Growth Inhibition Assay IC50=25.7136 μM SANGER
SW1573 Growth Inhibition Assay IC50=25.7785 μM SANGER
EW-24 Growth Inhibition Assay IC50=25.962 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=26.0312 μM SANGER
LU-65 Growth Inhibition Assay IC50=26.0452 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=26.0915 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=26.4114 μM SANGER
H4 Growth Inhibition Assay IC50=26.4243 μM SANGER
DU-4475 Growth Inhibition Assay IC50=27.1872 μM SANGER
HCT-116 Growth Inhibition Assay IC50=27.4349 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=27.6255 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=27.9617 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=28.2105 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=29.1431 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=29.3685 μM SANGER
TI-73 Growth Inhibition Assay IC50=29.4001 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=29.458 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=29.5505 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=29.6097 μM SANGER
KY821 Growth Inhibition Assay IC50=29.6433 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=29.8366 μM SANGER
NBsusSR Growth Inhibition Assay IC50=29.9904 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=30.5716 μM SANGER
NB14 Growth Inhibition Assay IC50=31.0446 μM SANGER
HCC1419 Growth Inhibition Assay IC50=31.24 μM SANGER
KG-1 Growth Inhibition Assay IC50=31.7429 μM SANGER
A2780 Growth Inhibition Assay IC50=31.8358 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=31.9861 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=32.2634 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=32.31 μM SANGER
SBC-5 Growth Inhibition Assay IC50=32.8511 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=33.4848 μM SANGER
COR-L88 Growth Inhibition Assay IC50=34.0741 μM SANGER
SW954 Growth Inhibition Assay IC50=34.0752 μM SANGER
COLO-684 Growth Inhibition Assay IC50=34.3404 μM SANGER
HCC70 Growth Inhibition Assay IC50=34.9514 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=34.961 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=35.8253 μM SANGER
YH-13 Growth Inhibition Assay IC50=35.92 μM SANGER
DJM-1 Growth Inhibition Assay IC50=36.8049 μM SANGER
KNS-62 Growth Inhibition Assay IC50=36.9438 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=37.8737 μM SANGER
SJRH30 Growth Inhibition Assay IC50=38.7341 μM SANGER
GP5d Growth Inhibition Assay IC50=38.8653 μM SANGER
SW1116 Growth Inhibition Assay IC50=39.2805 μM SANGER
COLO-800 Growth Inhibition Assay IC50=39.3638 μM SANGER
RD Growth Inhibition Assay IC50=39.5258 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=39.6916 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=40.108 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=40.5674 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=40.5932 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=40.6435 μM SANGER
SCC-4 Growth Inhibition Assay IC50=41.2137 μM SANGER
no-11 Growth Inhibition Assay IC50=41.7354 μM SANGER
HT-144 Growth Inhibition Assay IC50=42.0567 μM SANGER
MFM-223 Growth Inhibition Assay IC50=42.402 μM SANGER
ONS-76 Growth Inhibition Assay IC50=42.8018 μM SANGER
ES8 Growth Inhibition Assay IC50=43.3698 μM SANGER
T-24 Growth Inhibition Assay IC50=43.4369 μM SANGER
GAMG Growth Inhibition Assay IC50=43.4517 μM SANGER
LU-135 Growth Inhibition Assay IC50=44.0923 μM SANGER
HCC1187 Growth Inhibition Assay IC50=44.8262 μM SANGER
TE-1 Growth Inhibition Assay IC50=45.1654 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=45.4315 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=45.8952 μM SANGER
D-392MG Growth Inhibition Assay IC50=45.9256 μM SANGER
KALS-1 Growth Inhibition Assay IC50=46.7257 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=46.9952 μM SANGER
HSC-3 Growth Inhibition Assay IC50=47.3608 μM SANGER
KM-H2 Growth Inhibition Assay IC50=47.6007 μM SANGER
LoVo Growth Inhibition Assay IC50=48.1002 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=48.1871 μM SANGER
EW-11 Growth Inhibition Assay IC50=48.2348 μM SANGER
HCC2998 Growth Inhibition Assay IC50=48.6236 μM SANGER
J82 Growth Inhibition Assay IC50=48.7242 μM SANGER
ML-2 Growth Inhibition Assay IC50=49.4605 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=49.7117 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=49.8518 μM SANGER
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.001 μM. 26789553
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay, IC50 = 0.00154 μM. 23088644
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.002 μM. 26789553
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.003 μM. 23301703
KU812 Antiproliferative assay Antiproliferative activity against human KU812 cells, IC50 = 0.0034 μM. 21376587
Ba/F3 Function assay 48 hrs Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00352 μM. 30137981
HEK293 Function assay Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50 = 0.0037 μM. 20817538
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00371 μM. 30137981
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0039 μM. 26814890
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.004 μM. 26789553
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00482 μM. 30137981
HEK293 Function assay Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50 = 0.0052 μM. 20817538
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay, IC50 = 0.00634 μM. 23088644
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50 = 0.0065 μM. 21376587
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay, IC50 = 0.00838 μM. 23088644
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00921 μM. 30137981
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.0095 μM. 23301703
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay, IC50 = 0.0103 μM. 23088644
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0128 μM. 23301703
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50 = 0.015 μM. 23521020
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0158 μM. 23301703
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.016 μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.017 μM. 26789553
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0189 μM. 30137981
Ba/F Function assay Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50 = 0.02 μM. 20817538
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50 = 0.021 μM. 20817538
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay, IC50 = 0.021 μM. 23088644
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.021 μM. 26789553
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.022 μM. 23301703
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.022 μM. 26195136
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.023 μM. 26789553
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0242 μM. 23301703
BA/F3 Antiproliferative assay Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50 = 0.025 μM. 20817538
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.025 μM. 26789553
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0278 μM. 23301703
K562 Function assay 30 mins Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.028 μM. 28280261
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0296 μM. 30137981
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0299 μM. 23301703
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0369 μM. 30137981
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay, IC50 = 0.0386 μM. 23088644
K562 Function assay Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50 = 0.042 μM. 20817538
insect cells Function assay 30 mins Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0435 μM. 23301703
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.0546 μM. 26789553
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay, IC50 = 0.0607 μM. 23088644
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0616 μM. 30137981
BA/F3 Antiproliferative assay Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50 = 0.062 μM. 20817538
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.0652 μM. 23088644
A31 Function assay Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM. 20817538
A31 Function assay Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM. 20817538
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay, IC50 = 0.0872 μM. 23088644
K562 Function assay 30 mins Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.1 μM. 28280261
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.12 μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.12 μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.13 μM. 23301703
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.132 μM. 30137981
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay, IC50 = 0.15 μM. 23088644
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.15 μM. 23301703
GIST882 Antiproliferative assay Antiproliferative activity against human GIST882 cells, IC50 = 0.151 μM. 20817538
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay, IC50 = 0.159 μM. 23088644
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.16 μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.17 μM. 23301703
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.202 μM. 26789553
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.2153 μM. 23301703
GIST882 Function assay Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50 = 0.217 μM. 20817538
K562 Antiproliferative assay Antiproliferative activity against human imatinib-resistant K562 cells, IC50 = 0.26 μM. 21376587
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay, IC50 = 0.292 μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay, IC50 = 0.314 μM. 23088644
BA/F3 Function assay 72 hrs Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.47 μM. 26789553
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay, IC50 = 0.473 μM. 23088644
HEK293 Function assay Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50 = 0.677 μM. 20817538
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.7024 μM. 23301703
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay, IC50 = 0.775 μM. 23088644
M-NFS-60 Antiproliferative assay Antiproliferative activity against mouse M-NFS-60 cells, IC50 = 0.838 μM. 20817538
BA/F3 Function assay 72 hrs Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.87 μM. 26789553
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1 μM. 23301703
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.093 μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.1 μM. 26789553
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.2 μM. 23301703
BA/F3 Function assay 72 hrs Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.3 μM. 26789553
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.4 μM. 23301703
BA/F3 Function assay 72 hrs Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.4 μM. 26789553
NCI-H2286 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay, IC50 = 1.8 μM. 26191369
K562 Function assay 30 mins Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 1.8 μM. 28280261
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 2.1 μM. 26789553
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 2.262 μM. 30137981
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2.39 μM. 23521020
K562 Antiproliferative assay 72 hrs Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 2.4 μM. 24835982
MDA-MB-435S Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50 = 2.66 μM. 23521020
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 2.7 μM. 26814890
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 2.9 μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 3 μM. 23301703
NCI-H23 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50 = 3.05 μM. 23521020
HEL Antiproliferative assay 72 hrs Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 3.9 μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.1 μM. 26789553
CHL Antiproliferative assay 72 hrs Antiproliferative activity against human CHL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.2 μM. 26789553
CHO Function assay Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 4.7 μM. 23812503
T47D Antiproliferative assay 72 hrs Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.08 μM. 23521020
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 6.63 μM. 23521020
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.92 μM. 23521020
BJ Antiproliferative assay 72 hrs Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 12.8 μM. 24835982
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 14.41 μM. 23521020
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 15.1 μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 16 μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 21.1 μM. 23301703
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50 = 40.75 μM. 23088644
BA/F3 Antitumor assay 75 mg/kg 19 days Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as median survival time at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control 19572547
BA/F3 Antitumor assay 75 mg/kg 19 days Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as increase in mouse survival at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control 19572547
vascular smooth muscle cells Antiangiogenic assay 0.15 uM 72 hrs Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of cell growth at 0.15 uM after 72 hrs 22853993
vascular smooth muscle cells Antiangiogenic assay 10 to 15 uM 72 hrs Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of network formation at 10 to 15 uM after 72 hrs 22853993
HEK293 Function assay 0.1 to 1 uM 16 hrs Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting 26191369
HEK293 Function assay 0.1 to 1 uM 16 hrs Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting 26191369
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Features A selective inhibitor of native and mutant Bcr-Abl.
Targets
Bcr-Abl [1]
(Murine myeloid progenitor cells)
<30 nM
In vitro
In vitro Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of α-SMA and collagen in activated HSCs. Nilotinib induces apoptosis of HSCs, which is correlated with reduced bcl-2 expression, increases p53 expression, cleavage of PARP, as well as increases expression of PPARγ and TRAIL-R. Nilotinib also induces cell cycle arrest, accompanied by increased expression of p27 and downregulation of cyclin D1. Interestingly, Nilotinib not only inhibits activation of PDGFR, but also TGFRII through Src. Nilotinib significantly inhibits PDGF and TGFβ-simulated phosphorylation of ERK and Akt. Furthermore, PDGF- and TGFβ-activated phosphorylated form(s) of Abl in human HSCs are inhibited by Nilotinib. [2] Nilotinib inhibits most imatinib-resistant Bcr-Abl mutations, except for T315I. [3] Nilotinib inhibits PDGF-DD-mediated ERK1/2 activation, basal and PDGF-DD-mediated activation of PDGFRβ and Akt, and schwannoma proliferation. Nilotinib is more potent than imatinib, exerting its maximal inhibitory effect at concentrations lower than steady-state trough plasma levels. [4] Nilotinib also significantly reduces the expression levels of the genes for TGF-β1 and platelet-derived growth factor (PDGF). Nilotinib treatment also significantly inhibits the PDGF-induced proliferation of lung fibroblasts. [5] Nilotinib inhibits the proliferation of Ba/F3 cells expressing p210- and p190-Bcr-Abl, or K562 and Ku-812F cells with IC50 values ≤12 nM. [6]
Cell Research Cell lines Human primary Schwann and schwannoma cells
Concentrations 1-10 μM
Incubation Time 72 hours
Method Human primary Schwann and schwannoma cells are seeded on precoated 96-well plates. Nilotinib is added 40 minutes before stimulation with 100 ng/mL PDGF-DD, and cells are cultured for 72 hours (3 days). Because the half-life of Nilotinib is 18 hours, one-half of the originally added concentrations are added freshly every day. In addition to DAPI staining and determination of the total cell number, the more sensitive and accurate BrdU incorporation method is used to detect proliferating cells. Total cell amount (DAPI) and number of dividing cells (BrdU-positive) are blindly counted using an inverted fluorescent microscope and 200 × magnification. All cells in every well are counted. The total cell number per well differed between various cell batches and is 100–300 cells/well.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AMPKα / AMPKα / p-AMPKβ1 / AMPKγ2 / p-LKB1 / LKB1 / CaMKIIβ DNMT1 / DNMT3a / DNMT3b pABL1 / p-NF-κB1 / NF-κB / STAT3 / p-STAT3 / IL-1β / IL-6 / COX2 23677989
Growth inhibition assay Cell viability 23677989
In Vivo
In vivo Nilotinib reduces collagen deposition and α-SMA expression in CCl4 and BDL-induced fibrosis. Nilotinib could induce HSC undergoing apoptosis, which is correlated with downregulation of bcl-2. [2] Nilotinib attenuates the extent of lung injury and fibrosis. Nilotinib therapy significantly reduces the levels of hydroxyproline on days 14 and 21, which is accompanied by decreased expression levels of transforming growth factor (TGF)-β1 and PDGFRβ. [5] AMN107 prolongs survival of mice injected with Bcr-Abl-transformed hematopoietic cell lines or primary marrow cells, and prolongs survival in imatinib-resistant CML mouse models. [6]
Animal Research Animal Models Systemic 32D Bcr-Abl leukemia model in Female BALB/c mice, Bioluminescent Bcr-Abl model of CML in Female NOD-SCID mice and Bone marrow transplant Bcr-Abl model of CML in syngeneic Balb/c recipient mice
Dosages 75 mg/kg, 100 mg/kg
Administration Oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06409936 Not yet recruiting
CML Chronic Phase|Chronic Myeloid Leukemia Chronic Phase|Chronic Myeloid Leukemia BCR/ABL-Positive|Chronic Myeloid Leukemia
Gruppo Italiano Malattie EMatologiche dell''Adulto|Fundacion Espanola para la Curacion de la Leucemia Mieloide Cronica
September 2024 Phase 2
NCT05185947 Recruiting
Gynecologic Cancer|Gynecologic Neoplasms|Peritoneal Carcinomatosis|Peritoneal Neoplasms|Ovarian Cancer|Ovarian Neoplasms|Colorectal Cancer|Colorectal Neoplasms|Appendiceal Cancer|Appendiceal Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
October 13 2022 Phase 2
NCT04326933 Unknown status
Patients Diagnosed as Chronic Meyloid Leukemia
Assiut University
January 1 2020 --
NCT04002674 Recruiting
Dementia With Lewy Bodies
Georgetown University|National Institutes of Health (NIH)
July 1 2019 Phase 2

Chemical Information & Solubility

Molecular Weight 529.52 Formula

C28H22F3N7O

CAS No. 641571-10-0 SDF Download Nilotinib SDF
Smiles CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 52 mg/mL ( (98.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I would like to use AMN-107 for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?

Answer:
For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml.

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