Home Angiogenesis FGFR inhibitor - VEGFR inhibitor - Apoptosis related activator PD173074 For research use only.

PD173074

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

PD173074 Chemical Structure

PD173074 Chemical Structure

CAS No. 219580-11-7

Purity & Quality Control

PD173074 Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 Growth Inhibition Assay IC50=0.01225 μM SANGER
KG-1 Growth Inhibition Assay IC50=0.05129 μM SANGER
MFM-223 Growth Inhibition Assay IC50=0.21576 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.32984 μM SANGER
ECC10 Growth Inhibition Assay IC50=0.33898 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=0.34715 μM SANGER
AN3-CA Growth Inhibition Assay IC50=0.40133 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=0.54653 μM SANGER
RT-112 Growth Inhibition Assay IC50=0.54701 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.56289 μM SANGER
D-263MG Growth Inhibition Assay IC50=0.71159 μM SANGER
SW962 Growth Inhibition Assay IC50=0.78988 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.84623 μM SANGER
MFE-280 Growth Inhibition Assay IC50=0.85872 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.24464 μM SANGER
RS4-11 Growth Inhibition Assay IC50=1.33886 μM SANGER
DMS-114 Growth Inhibition Assay IC50=1.36737 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=1.47378 μM SANGER
DU-145 Growth Inhibition Assay IC50=1.58217 μM SANGER
A172 Growth Inhibition Assay IC50=1.70355 μM SANGER
SBC-1 Growth Inhibition Assay IC50=2.094 μM SANGER
H9 Growth Inhibition Assay IC50=2.14306 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=2.18394 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=2.21283 μM SANGER
HCC2218 Growth Inhibition Assay IC50=2.37939 μM SANGER
G-401 Growth Inhibition Assay IC50=2.47189 μM SANGER
MPP-89 Growth Inhibition Assay IC50=2.48364 μM SANGER
697 Growth Inhibition Assay IC50=2.65331 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=2.70747 μM SANGER
MG-63 Growth Inhibition Assay IC50=2.94262 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=3.03472 μM SANGER
G-402 Growth Inhibition Assay IC50=3.12727 μM SANGER
NKM-1 Growth Inhibition Assay IC50=3.13564 μM SANGER
RH-18 Growth Inhibition Assay IC50=3.19598 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=3.1969 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=3.23447 μM SANGER
GAMG Growth Inhibition Assay IC50=3.46576 μM SANGER
HH Growth Inhibition Assay IC50=3.47676 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=3.49855 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=3.50488 μM SANGER
NBsusSR Growth Inhibition Assay IC50=3.63969 μM SANGER
CHL-1 Growth Inhibition Assay IC50=3.65799 μM SANGER
LK-2 Growth Inhibition Assay IC50=3.67133 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=3.67873 μM SANGER
CTB-1 Growth Inhibition Assay IC50=3.80051 μM SANGER
ES5 Growth Inhibition Assay IC50=3.83637 μM SANGER
A204 Growth Inhibition Assay IC50=3.92075 μM SANGER
SW780 Growth Inhibition Assay IC50=3.92245 μM SANGER
EW-3 Growth Inhibition Assay IC50=3.98923 μM SANGER
A704 Growth Inhibition Assay IC50=4.28723 μM SANGER
LU-139 Growth Inhibition Assay IC50=4.31534 μM SANGER
CAL-72 Growth Inhibition Assay IC50=4.41746 μM SANGER
D-336MG Growth Inhibition Assay IC50=4.46817 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=4.5331 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=4.5481 μM SANGER
KM-H2 Growth Inhibition Assay IC50=4.55222 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=4.58283 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=4.87168 μM SANGER
L-363 Growth Inhibition Assay IC50=4.96665 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=5.2406 μM SANGER
HuO9 Growth Inhibition Assay IC50=5.38843 μM SANGER
NOS-1 Growth Inhibition Assay IC50=5.72927 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=5.95032 μM SANGER
SF126 Growth Inhibition Assay IC50=6.21406 μM SANGER
ML-2 Growth Inhibition Assay IC50=6.24977 μM SANGER
CHP-134 Growth Inhibition Assay IC50=6.25182 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=6.41733 μM SANGER
TE-12 Growth Inhibition Assay IC50=6.72671 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=6.73142 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=6.76626 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=6.91784 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=7.07764 μM SANGER
ME-180 Growth Inhibition Assay IC50=7.10404 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=7.37819 μM SANGER
HAL-01 Growth Inhibition Assay IC50=7.48341 μM SANGER
ES8 Growth Inhibition Assay IC50=7.69626 μM SANGER
DB Growth Inhibition Assay IC50=8.11504 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=8.48149 μM SANGER
COR-L88 Growth Inhibition Assay IC50=8.50981 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=8.52212 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=8.62157 μM SANGER
SW954 Growth Inhibition Assay IC50=8.69786 μM SANGER
TE-6 Growth Inhibition Assay IC50=8.75143 μM SANGER
D-283MED Growth Inhibition Assay IC50=9.06534 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=9.09607 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=9.29526 μM SANGER
HOS Growth Inhibition Assay IC50=9.35134 μM SANGER
ES4 Growth Inhibition Assay IC50=9.50595 μM SANGER
EW-13 Growth Inhibition Assay IC50=9.89055 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=9.94534 μM SANGER
CAS-1 Growth Inhibition Assay IC50=9.97659 μM SANGER
EM-2 Growth Inhibition Assay IC50=10.1393 μM SANGER
SW948 Growth Inhibition Assay IC50=10.1882 μM SANGER
OAW-42 Growth Inhibition Assay IC50=10.5267 μM SANGER
BE-13 Growth Inhibition Assay IC50=10.6576 μM SANGER
KU812 Growth Inhibition Assay IC50=10.7391 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=10.8901 μM SANGER
A2780 Growth Inhibition Assay IC50=11.0308 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=11.0737 μM SANGER
GOTO Growth Inhibition Assay IC50=11.2084 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=11.3837 μM SANGER
BHT-101 Growth Inhibition Assay IC50=11.4456 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=11.4947 μM SANGER
MCF7 Growth Inhibition Assay IC50=11.6167 μM SANGER
MKN45 Growth Inhibition Assay IC50=11.7993 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=11.9692 μM SANGER
YH-13 Growth Inhibition Assay IC50=12.0346 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=12.3845 μM SANGER
GR-ST Growth Inhibition Assay IC50=12.5295 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=12.791 μM SANGER
LXF-289 Growth Inhibition Assay IC50=13.0835 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=13.2704 μM SANGER
EW-16 Growth Inhibition Assay IC50=13.3187 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=13.4195 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=13.4547 μM SANGER
COLO-684 Growth Inhibition Assay IC50=13.5318 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=13.8109 μM SANGER
NB69 Growth Inhibition Assay IC50=13.9868 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=14.4453 μM SANGER
MKN7 Growth Inhibition Assay IC50=14.6676 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=15.1286 μM SANGER
A253 Growth Inhibition Assay IC50=15.3869 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=15.9094 μM SANGER
MEG-01 Growth Inhibition Assay IC50=15.9107 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=15.9376 μM SANGER
H4 Growth Inhibition Assay IC50=16.088 μM SANGER
LU-65 Growth Inhibition Assay IC50=16.3384 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=16.5165 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=16.5889 μM SANGER
CAL-120 Growth Inhibition Assay IC50=16.9879 μM SANGER
LU-134-A Growth Inhibition Assay IC50=17.3391 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=17.7127 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=17.9307 μM SANGER
MC116 Growth Inhibition Assay IC50=17.975 μM SANGER
UMC-11 Growth Inhibition Assay IC50=18.1788 μM SANGER
HCC1395 Growth Inhibition Assay IC50=18.4301 μM SANGER
no-10 Growth Inhibition Assay IC50=18.6388 μM SANGER
NY Growth Inhibition Assay IC50=19.0809 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=19.1252 μM SANGER
D-423MG Growth Inhibition Assay IC50=19.3952 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=19.7612 μM SANGER
DU-4475 Growth Inhibition Assay IC50=19.8852 μM SANGER
YKG-1 Growth Inhibition Assay IC50=19.962 μM SANGER
HCC1569 Growth Inhibition Assay IC50=20.2624 μM SANGER
TYK-nu Growth Inhibition Assay IC50=20.2847 μM SANGER
DEL Growth Inhibition Assay IC50=20.9808 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=21.3597 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=21.529 μM SANGER
CTV-1 Growth Inhibition Assay IC50=21.6172 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=22.6677 μM SANGER
D-566MG Growth Inhibition Assay IC50=22.7601 μM SANGER
EFO-27 Growth Inhibition Assay IC50=23.0651 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=23.8527 μM SANGER
KS-1 Growth Inhibition Assay IC50=24.2759 μM SANGER
8305C Growth Inhibition Assay IC50=24.4045 μM SANGER
A427 Growth Inhibition Assay IC50=25.0323 μM SANGER
COLO-800 Growth Inhibition Assay IC50=25.1061 μM SANGER
SJRH30 Growth Inhibition Assay IC50=25.3908 μM SANGER
MEL-HO Growth Inhibition Assay IC50=25.4319 μM SANGER
FTC-133 Growth Inhibition Assay IC50=25.8186 μM SANGER
SF295 Growth Inhibition Assay IC50=26.296 μM SANGER
SW1710 Growth Inhibition Assay IC50=26.4123 μM SANGER
EFM-19 Growth Inhibition Assay IC50=26.8145 μM SANGER
NB10 Growth Inhibition Assay IC50=28.2297 μM SANGER
TK10 Growth Inhibition Assay IC50=28.2399 μM SANGER
D-502MG Growth Inhibition Assay IC50=28.4 μM SANGER
EW-18 Growth Inhibition Assay IC50=28.4386 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=28.941 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=29.4557 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=29.5786 μM SANGER
A101D Growth Inhibition Assay IC50=29.6472 μM SANGER
WM-115 Growth Inhibition Assay IC50=29.7607 μM SANGER
HCC2157 Growth Inhibition Assay IC50=29.8807 μM SANGER
TE-9 Growth Inhibition Assay IC50=29.8865 μM SANGER
K-562 Growth Inhibition Assay IC50=30.0933 μM SANGER
SN12C Growth Inhibition Assay IC50=30.1426 μM SANGER
ESS-1 Growth Inhibition Assay IC50=30.4759 μM SANGER
K5 Growth Inhibition Assay IC50=30.764 μM SANGER
J82 Growth Inhibition Assay IC50=31.0897 μM SANGER
HOP-92 Growth Inhibition Assay IC50=31.1111 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=31.3296 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=31.361 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=31.8137 μM SANGER
A3-KAW Growth Inhibition Assay IC50=31.9243 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=32.0171 μM SANGER
KY821 Growth Inhibition Assay IC50=32.6884 μM SANGER
JVM-2 Growth Inhibition Assay IC50=32.9079 μM SANGER
Mo-T Growth Inhibition Assay IC50=33.1005 μM SANGER
IA-LM Growth Inhibition Assay IC50=33.275 μM SANGER
C8166 Growth Inhibition Assay IC50=33.3192 μM SANGER
TCCSUP Growth Inhibition Assay IC50=33.4307 μM SANGER
JEG-3 Growth Inhibition Assay IC50=33.4768 μM SANGER
MS-1 Growth Inhibition Assay IC50=33.5551 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=33.5725 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=34.0335 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=34.6395 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=34.7181 μM SANGER
SW900 Growth Inhibition Assay IC50=34.8115 μM SANGER
HCC2998 Growth Inhibition Assay IC50=35.1529 μM SANGER
A2058 Growth Inhibition Assay IC50=35.6061 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=36.2045 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=36.2294 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=36.4699 μM SANGER
SCC-9 Growth Inhibition Assay IC50=37.4027 μM SANGER
SF268 Growth Inhibition Assay IC50=38.3433 μM SANGER
HGC-27 Growth Inhibition Assay IC50=38.3711 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=38.7158 μM SANGER
KE-37 Growth Inhibition Assay IC50=38.9828 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=39.2502 μM SANGER
ES1 Growth Inhibition Assay IC50=39.385 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=39.9643 μM SANGER
SNU-449 Growth Inhibition Assay IC50=40.0764 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=40.1295 μM SANGER
HL-60 Growth Inhibition Assay IC50=40.9783 μM SANGER
DJM-1 Growth Inhibition Assay IC50=40.9799 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=41.0926 μM SANGER
U-2-OS Growth Inhibition Assay IC50=42.2641 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=42.4368 μM SANGER
LU-135 Growth Inhibition Assay IC50=42.5447 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=43.0493 μM SANGER
GT3TKB Growth Inhibition Assay IC50=43.2679 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=43.7816 μM SANGER
SAS Growth Inhibition Assay IC50=43.9534 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=43.9609 μM SANGER
JVM-3 Growth Inhibition Assay IC50=44.0533 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=44.5633 μM SANGER
SNB75 Growth Inhibition Assay IC50=44.6105 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=44.9328 μM SANGER
HCT-116 Growth Inhibition Assay IC50=44.9868 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=45.6368 μM SANGER
CAL-33 Growth Inhibition Assay IC50=45.9217 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=46.321 μM SANGER
HCC1187 Growth Inhibition Assay IC50=46.4255 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=46.5709 μM SANGER
T98G Growth Inhibition Assay IC50=47.547 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=47.683 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=47.727 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=48.1152 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=48.1853 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=48.2102 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=48.2726 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=48.2991 μM SANGER
SUM52 Antiproliferative assay 5 days Antiproliferative activity against human FGFR2-amplified SUM52 cells after 5 days by SRB assay, IC50 = 0.0123 μM. 28521156
RT112 Antiproliferative assay 72 hrs Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay, GI50 = 0.015 μM. 27599742
insect cells Function assay 10 mins Inhibition of recombinant full length human FGFR1 expressed in baculovirus infected insect cells in presence of [gamma-32P]ATP after 10 mins by scintillation counting based radioactive filter binding assay, IC50 = 0.0215 μM. 27914362
SW780 Antiproliferative assay 5 days Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay, IC50 = 0.0843 μM. 28521156
NIH/ 3T3 Function assay 5 mins Inhibition of VEGFR2 (unknown origin) overexpressed in mouse NIH/ 3T3 cells incubated for 5 mins followed by stimulation with VEGF for 5 mins by immunoblotting analysis, IC50 = 0.1 μM. 27326339
NCI-H520 Antiproliferative assay 7 days Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay, IC50 = 0.281 μM. 28521156
HUVEC Function assay 10 nM 14 hrs Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 10 nM after 14 hrs 16474387
HUVEC Function assay 100 nM 14 hrs Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 100 nM after 14 hrs 16474387
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.
Targets
FGFR1 [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)
~25 nM 100 nM-200 nM
In vitro
In vitro PD173074 is an ATP-competitive inhibitor of FGFR1 with Ki of ~40 nM. PD173074 is also an effective inhibitor of VEGFR2. Compared to FGFR1, PD173074 weakly inhibits the activities of Src, InsR, EGFR, PDGFR, MEK, and PKC with 1000-fold or greater IC50 values. PD173074 inhibits autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50 of 1-5 nM and 100-200 nM, respectively. [1] PD173074 inhibits FGF-2 promotion of granule neuron survival in a dose-dependent manner with IC50 of 12 nM, exhibiting 1,000-fold greater potency than that of SU 5402. [2] PD173074 specifically inhibits FGF-2-mediated effects on proliferation, differentiation, and MAPK activation in oligodendrocyte (OL) lineage cells. [3] PD173074 is active against the WT receptor and FGFR3 mutations in multiple myeloma (MM) cell lines. PD173074 also potently inhibits autophosphorylation of FGFR3 in a dose-dependent manner with IC50 of ~5 nM. PD173074 treatment potently reduces viability of FGFR3-expressing KMS11 and KMS18 cells with IC50 of <20 nM. Inhibition of aFGF-stimulated MM cell growth by PD173074 is highly correlated with the expression of FGFR3. PD173074 treatment completely abolishes NIH 3T3 transformation mediated by Y373C FGFR3 but not by Ras V12, demonstrating that PD173074 specifically targets FGFR3-mediated cell transformation and lacks nonspecific cytotoxic effect. PD173074 also induces functional maturation of KMS11 and KMS18 cells. [4]
Kinase Assay In vitro kinase inhibition assays
Assays using the full-length FGFR-1 kinase are performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl2, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction is initiated by the addition of [γ-32P]ATP (5 μM ATP containing 0.4 μCi of [γ-32P]ATP per incubation), and samples are incubated at 25°C for 10 minutes. The reaction is terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters are washed three times with 15% trichloroacetic acid, and the incorporation of [32P] into the glutamate tyrosine polymer substrate is determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. Nonspecific activity is defined as radioactivity retained on the filters following incubation of samples without enzyme. Specific activity is determined as total activity (enzyme plus buffer) minus nonspecific activity. The concentration of PD173074 that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically.
Cell Research Cell lines KMS11 and KMS18
Concentrations Dissolved in DMSO, final concentrations ~100 nM
Incubation Time 48 hours
Method Cells are incubated with increasing concentrations of PD173074 in the presence of aFGF/heparin for 48 hours. The percentage of viable cells is determined by MTT.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pFGFR2 / FGFR2 p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1 24968263
Growth inhibition assay Cell viability 24968263
In Vivo
In vivo Administration of PD173074 at 1 mg/kg/day or 2 mg/ka/day in mice can effectively block angiogenesis induced by either FGF or VEGF in a dose-dependent manner with no apparent toxicity. [1] PD173074 inhibits in vivo growth of mutant FGFR3-transfected NIH 3T3 cells in nude mice. Inhibition of FGFR3 by PD173074 delays tumor growth and increases survival of mice in a KMS11 xenograft myeloma model. [4] In the H-510 xenograft, oral aministration of PD173074 blocks tumor growth similar to that seen with single-agent cisplatin administration, increasing median survival compared with control sham-treated animals. In H-69 xenografts, PD173074 induces complete responses lasting >6 months in 50% of mice. These effects are correlated with increased apoptosis in excised tumors, but not a consequence of disrupted tumor vasculature. [5]
Animal Research Animal Models Swiss Webster mice with induced corneal angiogenesis
Dosages ~2 mg/kg/day
Administration Administered intraperitoneally

Chemical Information & Solubility

Molecular Weight 523.67 Formula

C28H41N7O3
CAS No. 219580-11-7 SDF Download PD173074 SDF
Smiles CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 105 mg/mL ( (200.5 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 105 mg/mL

Water : 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:
What is the half-life of PD173074(S1264) in vivo?

Answer:
According to literature research, PD173074 is given twice daily because it has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.

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