PD173074

Licensed by Pfizer Catalog No.S1264

PD173074 Chemical Structure

Molecular Weight(MW): 523.67

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.

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Cited by 46 Publications

Purity & Quality Control

Choose Selective FGFR Inhibitors

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.
Targets
FGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
~25 nM 100 nM-200 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 M{nUVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PvRWlEPTB;MD6wNVIzPSEQvF2= M{flUXNCVkeHUh?=
KG-1 M2DTT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPzOVZsUUN3ME2wMlA2OTJ7IN88US=> M13rbHNCVkeHUh?=
MFM-223 Mm\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzBTWM2OD1yLkKxOVc3KM7:TR?= M2nxU3NCVkeHUh?=
EoL-1-cell NIXPcY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwM{K5PFQh|ryP MVfTRW5ITVJ?
ECC10 NFn6W4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7qTWM2OD1yLkOzPFk5KM7:TR?= NXfvcHJ5W0GQR1XS
H-EMC-SS MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTJTWM2OD1yLkO0O|E2KM7:TR?= NYK0cIFwW0GQR1XS
AN3-CA NXK0SFloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkSxTWM2OD1yLkSwNVM{KM7:TR?= MW\TRW5ITVJ?
HuO-3N1 NY\EcYJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjjTWM2OD1yLkW0OlU{KM7:TR?= NHHCV|BUSU6JRWK=
RT-112 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nBR2lEPTB;MD61OFcxOSEQvF2= M1npVXNCVkeHUh?=
NEC8 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGSzVmpKSzVyPUCuOVYzQDlizszN M3:1RXNCVkeHUh?=
D-263MG MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjvcZNtUUN3ME2wMlcyOTV7IN88US=> NXv0[GJbW0GQR1XS
SW962 NHjEPGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonSTWM2OD1yLke4PVg5KM7:TR?= MknTV2FPT0WU
BV-173 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXNSIdKSzVyPUCuPFQ3OjNizszN NVm1[ZM2W0GQR1XS
MFE-280 NXjkO2FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnaOGNbUUN3ME2wMlg2QDd{IN88US=> MVnTRW5ITVJ?
HuH-7 NGC0WolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G2XmlEPTB;MT6yOFQ3PCEQvF2= M1ntOXNCVkeHUh?=
RS4-11 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFwM{O4PFYh|ryP M{TOR3NCVkeHUh?=
DMS-114 M{PtWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\INmlEPTB;MT6zOlc{PyEQvF2= M4\iNHNCVkeHUh?=
MSTO-211H NUD2[HJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NICxfIJKSzVyPUGuOFc{PzhizszN NUX5SYNzW0GQR1XS
DU-145 Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFwNUiyNVch|ryP MkPyV2FPT0WU
A172 NEXmOIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTFwN{CzOVUh|ryP NUezT2RpW0GQR1XS
SBC-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;N[GlEPTB;Mj6wPVQh|ryP NXHwfm5VW0GQR1XS
H9 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLkTWM2OD1{LkG0N|A3KM7:TR?= NID6PIpUSU6JRWK=
NCI-SNU-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJwMUizPVQh|ryP MWrTRW5ITVJ?
NCI-H720 NX3zSYp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{GyPGlEPTB;Mj6yNVI5OyEQvF2= NX63So5PW0GQR1XS
HCC2218 M{LyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPYeY1yUUN3ME2yMlM4QTN7IN88US=> MoroV2FPT0WU
G-401 NFjnUIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\LTWM2OD1{LkS3NVg6KM7:TR?= NUTtO3dIW0GQR1XS
MPP-89 M3K0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS0TWM2OD1{LkS4N|Y1KM7:TR?= NIf2NmVUSU6JRWK=
697 NIrLfWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTRTWM2OD1{Lk[1N|MyKM7:TR?= MXPTRW5ITVJ?
KARPAS-45 NIPGSmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJwN{C3OFch|ryP MWXTRW5ITVJ?
MG-63 M{nQS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LK[GlEPTB;Mj65OFI3OiEQvF2= NH[5cYdUSU6JRWK=
NTERA-S-cl-D1 M33ofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjuOYVQUUN3ME2zMlA{PDd{IN88US=> MnrhV2FPT0WU
G-402 NWLPOphDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jnPGlEPTB;Mz6xNlczPyEQvF2= NXTNeWJnW0GQR1XS
NKM-1 NWHBSIk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfKRVBLUUN3ME2zMlE{PTZ2IN88US=> M4\S[3NCVkeHUh?=
RH-18 NHLNSYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK5SZh6UUN3ME2zMlE6PTl6IN88US=> Mk\5V2FPT0WU
NCI-H1092 NVrBOph[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;pc5VKSzVyPUOuNVk3QSEQvF2= M{XTPXNCVkeHUh?=
RPMI-8226 NWi5SoQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3KXXVUUUN3ME2zMlI{PDR5IN88US=> NH7aflRUSU6JRWK=
GAMG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzyZnRKSzVyPUOuOFY2PzZizszN NFjSc4VUSU6JRWK=
HH M{HwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPMTWM2OD1|LkS3Olc3KM7:TR?= NV[xdFBZW0GQR1XS
RO82-W-1 NFL0SpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTNwNEm4OVUh|ryP NYTBbmJ4W0GQR1XS
CCRF-CEM NUG1PXZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYj3T5gxUUN3ME2zMlUxPDh6IN88US=> NFLqSYhUSU6JRWK=
NBsusSR MlvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HPNWlEPTB;Mz62N|k3QSEQvF2= MWTTRW5ITVJ?
CHL-1 NVr0SWhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL6RYNtUUN3ME2zMlY2Pzl7IN88US=> M2PZNnNCVkeHUh?=
LK-2 MojIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDSTlFKSzVyPUOuOlcyOzNizszN NGn1WmtUSU6JRWK=
Hs-578-T MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTNwNke4O|Mh|ryP MmXtV2FPT0WU
CTB-1 M2OxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTNwOECwOVEh|ryP NVS3TmV2W0GQR1XS
ES5 MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4qwZmlEPTB;Mz64N|Y{PyEQvF2= NVm0V4lwW0GQR1XS
A204 M1vIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTNwOUKwO|Uh|ryP MnvxV2FPT0WU
SW780 NF[zfm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrZTWM2OD1|LkmyNlQ2KM7:TR?= MVfTRW5ITVJ?
EW-3 NGTRRpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU[2b3NCUUN3ME2zMlk5QTJ|IN88US=> NX:yV4p7W0GQR1XS
A704 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vo[WlEPTB;ND6yPFczOyEQvF2= M4ezSnNCVkeHUh?=
LU-139 NXzXboRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[zWIFKSzVyPUSuN|E2OzRizszN Mnq2V2FPT0WU
CAL-72 NHL2VoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnWeYkxUUN3ME20MlQyPzR4IN88US=> MYXTRW5ITVJ?
D-336MG MlXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PZbmlEPTB;ND60OlgyPyEQvF2= MnfJV2FPT0WU
LAMA-84 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jYTWlEPTB;ND61N|MyKM7:TR?= M3\EbHNCVkeHUh?=
GI-ME-N NU\SUo1jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\kTWlEPTB;ND61OFgyKM7:TR?= NXrwRmFJW0GQR1XS
KM-H2 NVnkUFN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET5SYhKSzVyPUSuOVUzOjJizszN NEC3RotUSU6JRWK=
NCI-H209 NXr0TIR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULxdIY1UUN3ME20MlU5Ojh|IN88US=> NW[0O3dyW0GQR1XS
IGROV-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnK[oNEUUN3ME20Mlg4OTZ6IN88US=> M{K2UnNCVkeHUh?=
L-363 MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTRwOU[2OlUh|ryP M3OzUXNCVkeHUh?=
SK-MEL-3 NFnNRXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHn4Z2tKSzVyPUWuNlQxPiEQvF2= NWqyRpNKW0GQR1XS
HuO9 M1\KXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;reVNKSzVyPUWuN|g5PDNizszN MnfTV2FPT0WU
NOS-1 NGPvPXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnsSoxKSzVyPUWuO|I6OjdizszN M{DKbXNCVkeHUh?=
NCI-H1770 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3LbpBIUUN3ME21Mlk2ODN{IN88US=> MXzTRW5ITVJ?
SF126 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTZwMkG0NFYh|ryP Mm\yV2FPT0WU
ML-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S1cWlEPTB;Nj6yOFk4PyEQvF2= MXHTRW5ITVJ?
CHP-134 NU\3doQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnqzTWM2OD14LkK1NVgzKM7:TR?= MmL5V2FPT0WU
NCI-H1355 M3zZTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlG2TWM2OD14LkSxO|M{KM7:TR?= MVjTRW5ITVJ?
TE-12 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTZwN{K2O|Eh|ryP M323bHNCVkeHUh?=
A4-Fuk M3m0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVj4V4JRUUN3ME22Mlc{OTR{IN88US=> NEnLO2hUSU6JRWK=
MV-4-11 Ml[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD0e4RDUUN3ME22Mlc3PjJ4IN88US=> MnHDV2FPT0WU
SK-UT-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDKU3dKSzVyPU[uPVE4QDRizszN MYXTRW5ITVJ?
J-RT3-T3-5 NUfoOoo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTdwMEe3OlQh|ryP NWCz[5NvW0GQR1XS
ME-180 M2m3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX2VFZKSzVyPUeuNVA1ODRizszN NFjaXINUSU6JRWK=
SK-MEL-28 NGTnO3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP5To1KSzVyPUeuN|c5OTlizszN NWj6VYRUW0GQR1XS
HAL-01 NHH4cndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnRNll{UUN3ME23MlQ5OzRzIN88US=> MVvTRW5ITVJ?
ES8 NEmwUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v6PWlEPTB;Nz62PVYzPiEQvF2= MUnTRW5ITVJ?
DB NV7HRZk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWriXWQxUUN3ME24MlEyPTB2IN88US=> MkfWV2FPT0WU
SK-NEP-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRThwNEixOFkh|ryP MVPTRW5ITVJ?
COR-L88 NUDjPVh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2SwTGlEPTB;OD61NFk5OSEQvF2= NUfDdVdFW0GQR1XS
LB1047-RCC M3G5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRThwNUKyNVIh|ryP M2SyOXNCVkeHUh?=
NCI-H520 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHiS2ZtUUN3ME24MlYzOTV5IN88US=> MnG4V2FPT0WU
SW954 M4\XSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfkTGtKSzVyPUiuOlk4QDZizszN MlPpV2FPT0WU
TE-6 NWjkTZJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfWUWlKSzVyPUiuO|UyPDNizszN Mn[4V2FPT0WU
D-283MED MlHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\M[mlEPTB;OT6wOlU{PCEQvF2= M4fPUXNCVkeHUh?=
DBTRG-05MG MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\2VolKSzVyPUmuNFk3ODdizszN MYHTRW5ITVJ?
NCI-H446 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjUXJc4UUN3ME25MlI6PTJ4IN88US=> Mn62V2FPT0WU
HOS NUi3VIdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHMcVJwUUN3ME25MlM2OTN2IN88US=> MljPV2FPT0WU
ES4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTlwNUC1PVUh|ryP NH7ocXhUSU6JRWK=
EW-13 M1Hmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13LRWlEPTB;OT64PVA2PSEQvF2= MX3TRW5ITVJ?
IST-MES1 NH3oOFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzvWYRKSzVyPUmuPVQ2OzRizszN M3LwPHNCVkeHUh?=
CAS-1 NUO2PIhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLYTWM2OD17Lkm3OlU6KM7:TR?= NGPWW2FUSU6JRWK=
EM-2 MlXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTsb4V[UUN3ME2xNE4yOzl|IN88US=> MXTTRW5ITVJ?
SW948 NYjiNmZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PRRmlEPTB;MUCuNVg5OiEQvF2= MV;TRW5ITVJ?
OAW-42 NFHuTGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TERWlEPTB;MUCuOVI3PyEQvF2= MWHTRW5ITVJ?
BE-13 NIHzZZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVv6XIViUUN3ME2xNE43PTd4IN88US=> NGHB[|ZUSU6JRWK=
KU812 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G5U2lEPTB;MUCuO|M6OSEQvF2= MmnPV2FPT0WU
SK-MEL-30 M1u1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFyLki5NFEh|ryP NXj2S203W0GQR1XS
A2780 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[5VmlEPTB;MUGuNFMxQCEQvF2= NFvTS|JUSU6JRWK=
TGBC24TKB MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLiTVRVUUN3ME2xNU4xPzN5IN88US=> M4LWOHNCVkeHUh?=
GOTO NXPEWVh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXTSVFDUUN3ME2xNU4zODh2IN88US=> NYPaOmRKW0GQR1XS
NCI-H526 Mk\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn23TWM2OD1zMT6zPFM4KM7:TR?= M3fZdnNCVkeHUh?=
BHT-101 NVizdFI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTFzLkS0OVYh|ryP NGfF[ppUSU6JRWK=
NCI-H1155 NWfVR|FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmq3TWM2OD1zMT60PVQ4KM7:TR?= MlnYV2FPT0WU
MCF7 NYLlcJFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37BTmlEPTB;MUGuOlE3PyEQvF2= Ml3uV2FPT0WU
MKN45 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\5TWM2OD1zMT63PVk{KM7:TR?= NVP5bZBLW0GQR1XS
MOLT-16 Mkj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrqN|hDUUN3ME2xNU46Pjl{IN88US=> Mo\pV2FPT0WU
YH-13 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDqTWM2OD1zMj6wN|Q3KM7:TR?= MULTRW5ITVJ?
P12-ICHIKAWA M1LkWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHf1T3ZKSzVyPUGyMlM5PDVizszN M4[yfXNCVkeHUh?=
GR-ST MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn73TWM2OD1zMj61Nlk2KM7:TR?= NEXNcVZUSU6JRWK=
CAKI-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoftTWM2OD1zMj63PVEh|ryP NWDxWo45W0GQR1XS
LXF-289 NVrsc4U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnQO4dKSzVyPUGzMlA5OzVizszN NEnObIRUSU6JRWK=
MHH-PREB-1 M4X3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;mRpFkUUN3ME2xN{4zPzB2IN88US=> M3jFUnNCVkeHUh?=
EW-16 NGfOZ21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPoXYZKSzVyPUGzMlMyQDdizszN M3\R[XNCVkeHUh?=
NCI-H82 M2rwWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\1RY5KSzVyPUGzMlQyQTVizszN MmHLV2FPT0WU
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LCLC-97TM1 NWnR[oIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLDSGlOUUN3ME2xOk42QDh7IN88US=> MYPTRW5ITVJ?
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KARPAS-299 NH\DN4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTJzLkWyPUDPxE1? MXjTRW5ITVJ?
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NCI-H2452 NUnxcVhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnsXHh3UUN3ME2yNk43Pjd5IN88US=> NY[3VJNlW0GQR1XS
D-566MG MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJ{Lke2NFEh|ryP MU\TRW5ITVJ?
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NCI-H596 NG\UTotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJ|Lki1Nlch|ryP M1ewb3NCVkeHUh?=
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8305C NHnYe|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37PNmlEPTB;MkSuOFA1PSEQvF2= M4nIbnNCVkeHUh?=
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SW1710 MonSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTJ4LkSxNlMh|ryP M1XTbXNCVkeHUh?=
EFM-19 NIDFenhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojxTWM2OD1{Nj64NVQ2KM7:TR?= MX\TRW5ITVJ?
NB10 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e4VGlEPTB;MkiuNlI6PyEQvF2= MULTRW5ITVJ?
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D-502MG M2Sw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJ6LkSg{txO MnfKV2FPT0WU
EW-18 MlPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJ6LkSzPFYh|ryP MU\TRW5ITVJ?
VMRC-RCZ M1nCemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ6Lkm0NUDPxE1? M3fkfHNCVkeHUh?=
Ca9-22 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\3RWlEPTB;MkmuOFU2PyEQvF2= NGj4[FhUSU6JRWK=
KYSE-70 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnnd5JKSzVyPUK5MlU4QDZizszN MY\TRW5ITVJ?
A101D MnjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTJ7Lk[0O|Ih|ryP MnLEV2FPT0WU
WM-115 NHi3bVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJ7Lke2NFch|ryP MVnTRW5ITVJ?
HCC2157 NF\LdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7ETWM2OD1{OT64PFA4KM7:TR?= MYLTRW5ITVJ?
TE-9 NGrscotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJ7Lki4OlUh|ryP Mk\0V2FPT0WU
K-562 MkHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTNyLkC5N|Mh|ryP M32ybXNCVkeHUh?=
SN12C M4Do[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v0dGlEPTB;M{CuNVQzPiEQvF2= NWjsPFN7W0GQR1XS
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J82 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XDOmlEPTB;M{GuNFg6PyEQvF2= MmPsV2FPT0WU
HOP-92 M3jqfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LZc2lEPTB;M{GuNVEyOSEQvF2= NYPhUGJZW0GQR1XS
NCI-H2228 NWnQUVU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnleVFEUUN3ME2zNU4{Ojl4IN88US=> M3XjeXNCVkeHUh?=
OCI-AML2 M4rWNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTNzLkO2NUDPxE1? MVzTRW5ITVJ?
NCI-SNU-5 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DafWlEPTB;M{GuPFE{PyEQvF2= MUfTRW5ITVJ?
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LCLC-103H Mlu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjLOJVKSzVyPUOyMlAyPzFizszN NXPZfHpkW0GQR1XS
KY821 NWXOWY81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTN{Lk[4PFQh|ryP NWnTNZFzW0GQR1XS
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Mo-T MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3foOGlEPTB;M{OuNVAxPSEQvF2= MnTsV2FPT0WU
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C8166 NVTpbFBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTN|LkOxPVIh|ryP M4[1e3NCVkeHUh?=
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MS-1 M3qwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[yUWlEPTB;M{OuOVU2OSEQvF2= MkPsV2FPT0WU
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KYSE-520 NHP5OY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPVNYdmUUN3ME2zOE44OThzIN88US=> M3XmWHNCVkeHUh?=
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HCC2998 NH3keJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHM[2dKSzVyPUO1MlE2OjlizszN NVLhcJBlW0GQR1XS
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OVCAR-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NESyTWxKSzVyPUO2MlIxPDVizszN NEDoV2dUSU6JRWK=
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CAPAN-1 M3XObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TpdWlEPTB;M{[uOFY6QSEQvF2= M1XwdnNCVkeHUh?=
SCC-9 MkXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljVTWM2OD1|Nz60NFI4KM7:TR?= Mn;EV2FPT0WU
SF268 NFyzR5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H2XmlEPTB;M{iuN|Q{OyEQvF2= NHjUVHBUSU6JRWK=
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KE-37 Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\hcHR6UUN3ME2zPE46QDJ6IN88US=> MVvTRW5ITVJ?
MOLT-13 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN7LkK1NFIh|ryP M3[5VnNCVkeHUh?=
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SNU-449 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTRyLkC3OlQh|ryP MmfQV2FPT0WU
KYSE-510 MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPPfmFKSzVyPUSwMlEzQTVizszN NHnTdZFUSU6JRWK=
HL-60 NYLXS2psT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHGWoltUUN3ME20NE46Pzh|IN88US=> NUjiOI5JW0GQR1XS
DJM-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnlR4ZKSzVyPUSwMlk4QTlizszN MWPTRW5ITVJ?
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U-2-OS M3T5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTR{LkK2OFEh|ryP MXLTRW5ITVJ?
NCI-H2030 NFflO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3oXYFKSzVyPUSyMlQ{PjhizszN NITPRXZUSU6JRWK=
LU-135 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHCXmV7UUN3ME20Nk42PDR5IN88US=> NWH1VmFqW0GQR1XS
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GT3TKB MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXaflZSUUN3ME20N{4zPjd7IN88US=> NX\jSmtTW0GQR1XS
RPMI-2650 M2XpTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTR|Lke4NVYh|ryP M{\CPHNCVkeHUh?=
SAS NHnqdndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfrTWM2OD12Mz65OVM1KM7:TR?= Mon4V2FPT0WU
MDA-MB-231 NHrPdJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PKWWlEPTB;NEOuPVYxQSEQvF2= NHfIR2xUSU6JRWK=
JVM-3 NX63V2hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoSyTWM2OD12ND6wOVM{KM7:TR?= NX3R[2VsW0GQR1XS
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SNB75 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG3NYg{UUN3ME20OE43OTB3IN88US=> MWrTRW5ITVJ?
NCI-H441 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOzZ4pKSzVyPUS0Mlk{OjhizszN Ml[0V2FPT0WU
HCT-116 MkHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{O3T2lEPTB;NESuPVg3QCEQvF2= NUflXXRzW0GQR1XS
NCI-H226 NX;pS21sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTR3Lk[zOlgh|ryP NH\kZmRUSU6JRWK=
CAL-33 MmTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorXTWM2OD12NT65NlE4KM7:TR?= MWnTRW5ITVJ?
NCI-H1437 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTR4LkOyNUDPxE1? NHXHb4xUSU6JRWK=
HCC1187 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOzXnJKSzVyPUS2MlQzPTVizszN M4DMOHNCVkeHUh?=
NUGC-3 NH\ucWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXBTWM2OD12Nj61O|A6KM7:TR?= MmrQV2FPT0WU
T98G MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f3[WlEPTB;NEeuOVQ4KM7:TR?= Mlj1V2FPT0WU
OVCAR-8 MnjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\iU2lEPTB;NEeuOlg{KM7:TR?= MkDLV2FPT0WU
LB2241-RCC MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfyTWM2OD12Nz63Nlch|ryP MVjTRW5ITVJ?
NCI-H358 NEDOS3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXvTWM2OD12OD6xNVUzKM7:TR?= MXHTRW5ITVJ?
PANC-08-13 NH\jWXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHOTWM2OD12OD6xPFU{KM7:TR?= NVPxUWZQW0GQR1XS
KP-N-YN M4XmXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3m1WGlEPTB;NEiuNlExOiEQvF2= NFn5cYtUSU6JRWK=
NCI-H1755 M1TvO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXUOmNbUUN3ME20PE4zPzJ4IN88US=> NEPWXZBUSU6JRWK=
NCI-N87 M1TtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nYc2lEPTB;NEiuNlk6OSEQvF2= NV3PXFVxW0GQR1XS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pFGFR2 / FGFR2 ; 

PubMed: 24968263     


PD173074 and MK2461 inhibit FGFR2 phosphorylation. Cells were treated for 1 hour with a titration of PD173074 as described in Materials and methods. Lysates were prepared and 50 ug protein was subjected to SDS-PAGE and western blotting with phospho Y653/654 FGFR and MAB6841 total FGFR2 antibody.

p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1; 

PubMed: 24968263     


Time course of inhibition for multiple signaling proteins. NCI-H716 cells were treated with 100 nM PD173074 for the indicated times and signaling pathways were analyzed by SDS PAGE and western blotting. 100 nM PD173074 was selected because this amount caused full inhibition of pERK at the 2 hour time point. “p” indicates phosphoprotein, and the phosphorylation sites are listed in Methods. Terminology on the right side of figure groups proteins according to the time at which inhibition or protein loss occurs.

24968263
Growth inhibition assay
Cell viability; 

PubMed: 24968263     


B. PD173074 and MK2461 inhibit NCI-H716 cell growth. Cell lines were plated at 4000 cells/well and incubated overnight. NCI-H716 cells were treated with a titration of PD173074 as described in Materials and Methods. Cell growth was measured with Vialight reagent, and growth was presented relative to untreated cells. C. PD173074 and MK2461 selectively inhibit growth of NCI-H716 cells. Colon cancer cell lines listed were plated at 4000 cells/well and 24 hours later were treated with a titration of compounds. 4 days later cell growth was measured with vialight and IC50s were calculated from graph pad prism. 

24968263
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]

Protocol

Kinase Assay:[1]
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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:[4]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Swiss Webster mice with induced corneal angiogenesis
  • Formulation: Prepared in sterile fashion
  • Dosages: ~2 mg/kg/day
  • Administration: Administered intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (190.95 mM)
Ethanol 100 mg/mL (190.95 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 523.67
Formula

C28H41N7O3

CAS No. 219580-11-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID