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 30 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 Mni5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PMeGlEPTB;MD6wNVIzPSEQvF2= NIr4PFNUSU6JRWK=
KG-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3vTWM2OD1yLkC1NVI6KM7:TR?= MnPvV2FPT0WU
MFM-223 MlLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1KyR2lEPTB;MD6yNVU4PiEQvF2= NEi0TZhUSU6JRWK=
EoL-1-cell NXTjSHl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HlWWlEPTB;MD6zNlk5PCEQvF2= MYXTRW5ITVJ?
ECC10 M4fWNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mor1TWM2OD1yLkOzPFk5KM7:TR?= MVjTRW5ITVJ?
H-EMC-SS NYLB[pBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnMfYdLUUN3ME2wMlM1PzF3IN88US=> MWHTRW5ITVJ?
AN3-CA MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwNECxN|Mh|ryP NW\DXW9DW0GQR1XS
HuO-3N1 NXzHPGtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPqTWM2OD1yLkW0OlU{KM7:TR?= MkLGV2FPT0WU
RT-112 M3;yUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwNUS3NFEh|ryP MUfTRW5ITVJ?
NEC8 NVzT[3JrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwNU[yPFkh|ryP Mor3V2FPT0WU
D-263MG MofxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDMOnU6UUN3ME2wMlcyOTV7IN88US=> NUjrV4xyW0GQR1XS
SW962 MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvsTWM2OD1yLke4PVg5KM7:TR?= MnLsV2FPT0WU
BV-173 NV;IV|V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHq4ZYNKSzVyPUCuPFQ3OjNizszN NGjibWFUSU6JRWK=
MFE-280 NFqz[3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TiXmlEPTB;MD64OVg4OiEQvF2= NGnkZYNUSU6JRWK=
HuH-7 MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDUTWM2OD1zLkK0OFY1KM7:TR?= NYHPd5JJW0GQR1XS
RS4-11 NHrPV4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFwM{O4PFYh|ryP NGPpXIZUSU6JRWK=
DMS-114 NXHuVZZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTFwM{[3N|ch|ryP M325NHNCVkeHUh?=
MSTO-211H Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPFZ5pKSzVyPUGuOFc{PzhizszN NEjjc5lUSU6JRWK=
DU-145 NIr1[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu1V|VYUUN3ME2xMlU5OjF5IN88US=> NIXwS5JUSU6JRWK=
A172 NVHNNWZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLRfoR3UUN3ME2xMlcxOzV3IN88US=> M4L5S3NCVkeHUh?=
SBC-1 M1XE[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTJwMEm0JO69VQ>? NEDQVGFUSU6JRWK=
H9 NXXucItmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml73TWM2OD1{LkG0N|A3KM7:TR?= MX;TRW5ITVJ?
NCI-SNU-1 NFTOPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj4TWM2OD1{LkG4N|k1KM7:TR?= M{GyUnNCVkeHUh?=
NCI-H720 NV\vNWg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPzW3FKSzVyPUKuNlEzQDNizszN MoSyV2FPT0WU
HCC2218 NUDxb4ozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJwM{e5N|kh|ryP NGnXZWdUSU6JRWK=
G-401 NXHOU|Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z1[WlEPTB;Mj60O|E5QSEQvF2= M3XYPXNCVkeHUh?=
MPP-89 MnLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHWTWM2OD1{LkS4N|Y1KM7:TR?= MkTyV2FPT0WU
697 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD2VG9MUUN3ME2yMlY2OzNzIN88US=> MXzTRW5ITVJ?
KARPAS-45 MmGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLOTWM2OD1{LkewO|Q4KM7:TR?= MofNV2FPT0WU
MG-63 MofJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTJwOUSyOlIh|ryP MUPTRW5ITVJ?
NTERA-S-cl-D1 NVO1cXFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTNwMEO0O|Ih|ryP NXzxcJM1W0GQR1XS
G-402 NVyxcWlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DaTmlEPTB;Mz6xNlczPyEQvF2= NIq3cXZUSU6JRWK=
NKM-1 M13a[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjvWY04UUN3ME2zMlE{PTZ2IN88US=> NGnoWWdUSU6JRWK=
RH-18 NXzofm84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfzTWM2OD1|LkG5OVk5KM7:TR?= MUHTRW5ITVJ?
NCI-H1092 NV[1eFZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTNwMUm2PUDPxE1? MWLTRW5ITVJ?
RPMI-8226 M{PH[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPQTWM2OD1|LkKzOFQ4KM7:TR?= NHrpNGpUSU6JRWK=
GAMG M{TOeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnriTWM2OD1|LkS2OVc3KM7:TR?= M4rHd3NCVkeHUh?=
HH NFTZd45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTNwNEe2O|Yh|ryP MXnTRW5ITVJ?
RO82-W-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHHRoxKSzVyPUOuOFk5PTVizszN MlrJV2FPT0WU
CCRF-CEM MnjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG4TWM2OD1|LkWwOFg5KM7:TR?= NEfXd3dUSU6JRWK=
NBsusSR NIPhe5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3mTWM2OD1|Lk[zPVY6KM7:TR?= MWXTRW5ITVJ?
CHL-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDMTWM2OD1|Lk[1O|k6KM7:TR?= NHLvVJJUSU6JRWK=
LK-2 MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG4cllXUUN3ME2zMlY4OTN|IN88US=> NWHFS2tyW0GQR1XS
Hs-578-T NXnsN29IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVy4SWpmUUN3ME2zMlY4QDd|IN88US=> M2\se3NCVkeHUh?=
CTB-1 M4HCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLnPYtKSzVyPUOuPFAxPTFizszN NYHsdIE6W0GQR1XS
ES5 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXSN5lKSzVyPUOuPFM3OzdizszN MVTTRW5ITVJ?
A204 M2\WbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPZTWM2OD1|LkmyNFc2KM7:TR?= M{\2TnNCVkeHUh?=
SW780 NGjjUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzITWM2OD1|LkmyNlQ2KM7:TR?= Ml\uV2FPT0WU
EW-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV71ZWppUUN3ME2zMlk5QTJ|IN88US=> MXnTRW5ITVJ?
A704 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2i4W2lEPTB;ND6yPFczOyEQvF2= Ml7kV2FPT0WU
LU-139 NF[4VnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL5PVlKSzVyPUSuN|E2OzRizszN M4\QfHNCVkeHUh?=
CAL-72 MmTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r1b2lEPTB;ND60NVc1PiEQvF2= MXTTRW5ITVJ?
D-336MG M2HNS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrTcJlTUUN3ME20MlQ3QDF5IN88US=> M1TISHNCVkeHUh?=
LAMA-84 M2rrNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrWV3J[UUN3ME20MlU{OzFizszN MV3TRW5ITVJ?
GI-ME-N NUTZb3NoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnTOG4zUUN3ME20MlU1QDFizszN M4SwRnNCVkeHUh?=
KM-H2 NYTYSYhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVi0eFB{UUN3ME20MlU2OjJ{IN88US=> M3;hd3NCVkeHUh?=
NCI-H209 Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jud2lEPTB;ND61PFI5OyEQvF2= Mmr1V2FPT0WU
IGROV-1 NYjk[WpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXpNZY4UUN3ME20Mlg4OTZ6IN88US=> M{[xd3NCVkeHUh?=
L-363 MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf4TWM2OD12Lkm2OlY2KM7:TR?= NFewWG1USU6JRWK=
SK-MEL-3 NIjtfnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rZ[mlEPTB;NT6yOFA3KM7:TR?= NHXleGNUSU6JRWK=
HuO9 NFPpfmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWCzcZdOUUN3ME21MlM5QDR|IN88US=> NXnrNnZYW0GQR1XS
NOS-1 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV65O2RDUUN3ME21MlczQTJ5IN88US=> MXfTRW5ITVJ?
NCI-H1770 Mo\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTOdZpGUUN3ME21Mlk2ODN{IN88US=> MlLSV2FPT0WU
SF126 NV3y[YpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTZwMkG0NFYh|ryP NFH6b4dUSU6JRWK=
ML-2 NE\rSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYntR4FnUUN3ME22MlI1QTd5IN88US=> MWHTRW5ITVJ?
CHP-134 NWPTVJp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXtR3pKSzVyPU[uNlUyQDJizszN MVrTRW5ITVJ?
NCI-H1355 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2i5NGlEPTB;Nj60NVc{OyEQvF2= NEHDNppUSU6JRWK=
TE-12 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTZwN{K2O|Eh|ryP NWrSUohtW0GQR1XS
A4-Fuk M1HTTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTZwN{OxOFIh|ryP MYDTRW5ITVJ?
MV-4-11 M{TycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvJTWM2OD14Lke2OlI3KM7:TR?= MYLTRW5ITVJ?
SK-UT-1 MnLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTZwOUG3PFQh|ryP NXHtNWF7W0GQR1XS
J-RT3-T3-5 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HWR2lEPTB;Nz6wO|c3PCEQvF2= NE\uWmJUSU6JRWK=
ME-180 NYHrS21uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfzTWM2OD15LkGwOFA1KM7:TR?= MoTGV2FPT0WU
SK-MEL-28 M1f3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fZVWlEPTB;Nz6zO|gyQSEQvF2= NFTQcYlUSU6JRWK=
HAL-01 M1T3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTdwNEizOFEh|ryP NWC3T2p1W0GQR1XS
ES8 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILkcYVKSzVyPUeuOlk3OjZizszN NUjUZlRsW0GQR1XS
DB MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3UTWM2OD16LkGxOVA1KM7:TR?= NF\CV3hUSU6JRWK=
SK-NEP-1 NYPab21RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVKzZYpiUUN3ME24MlQ5OTR7IN88US=> NYXGZ3VyW0GQR1XS
COR-L88 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4frSGlEPTB;OD61NFk5OSEQvF2= M4nwNHNCVkeHUh?=
LB1047-RCC M{Hlemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jkbmlEPTB;OD61NlIyOiEQvF2= MXnTRW5ITVJ?
NCI-H520 NVvCWZZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRThwNkKxOVch|ryP Mo[1V2FPT0WU
SW954 MofLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PHS2lEPTB;OD62PVc5PiEQvF2= M3PwSXNCVkeHUh?=
TE-6 NGmzeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfzdYhKSzVyPUiuO|UyPDNizszN MVzTRW5ITVJ?
D-283MED MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLBTWM2OD17LkC2OVM1KM7:TR?= M{j3d3NCVkeHUh?=
DBTRG-05MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFiz[XJKSzVyPUmuNFk3ODdizszN NUDyPVZ3W0GQR1XS
NCI-H446 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXu5T4lQUUN3ME25MlI6PTJ4IN88US=> M1zwOnNCVkeHUh?=
HOS Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHPTWM2OD17LkO1NVM1KM7:TR?= NF;WSJhUSU6JRWK=
ES4 NEO3WIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHXTWM2OD17LkWwOVk2KM7:TR?= NFTaSZhUSU6JRWK=
EW-13 M4n3VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j4PGlEPTB;OT64PVA2PSEQvF2= NVi1SYU2W0GQR1XS
IST-MES1 M4nFe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\ESWlEPTB;OT65OFU{PCEQvF2= MXzTRW5ITVJ?
CAS-1 NHHMTZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjlT|ZKSzVyPUmuPVc3PTlizszN NH;vWWxUSU6JRWK=
EM-2 NVv2PYFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFe3R2dKSzVyPUGwMlE{QTNizszN Ml32V2FPT0WU
SW948 NH7FNJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL2VmpNUUN3ME2xNE4yQDh{IN88US=> M4Xmd3NCVkeHUh?=
OAW-42 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7zWopKUUN3ME2xNE42OjZ5IN88US=> Mny3V2FPT0WU
BE-13 NX7RN3BzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrWPIpMUUN3ME2xNE43PTd4IN88US=> M3Plb3NCVkeHUh?=
KU812 NFvsSlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fxeWlEPTB;MUCuO|M6OSEQvF2= Mn7YV2FPT0WU
SK-MEL-30 NHvWbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYezVJdWUUN3ME2xNE45QTBzIN88US=> MkTEV2FPT0WU
A2780 NF7vboFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjRc4NKSzVyPUGxMlA{ODhizszN NUXEUWx1W0GQR1XS
TGBC24TKB MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\GS2lEPTB;MUGuNFc{PyEQvF2= NFLqcXVUSU6JRWK=
GOTO NHrVTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\iNWlEPTB;MUGuNlA5PCEQvF2= M2LwdnNCVkeHUh?=
NCI-H526 NFfuRmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnCfmR{UUN3ME2xNU4{QDN5IN88US=> MnT2V2FPT0WU
BHT-101 NVvEPGhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFzLkS0OVYh|ryP NGqzXXhUSU6JRWK=
NCI-H1155 MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jBOGlEPTB;MUGuOFk1PyEQvF2= M4fISnNCVkeHUh?=
MCF7 NID3e45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXwPY9KSzVyPUGxMlYyPjdizszN NG\wS5pUSU6JRWK=
MKN45 NEnZd2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rHV2lEPTB;MUGuO|k6OyEQvF2= MXrTRW5ITVJ?
MOLT-16 NVSyPYVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vDS2lEPTB;MUGuPVY6OiEQvF2= Mo\jV2FPT0WU
YH-13 M1jubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7QTWM2OD1zMj6wN|Q3KM7:TR?= M1PsOnNCVkeHUh?=
P12-ICHIKAWA MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\uTWM2OD1zMj6zPFQ2KM7:TR?= M{Lid3NCVkeHUh?=
GR-ST M3:zfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrEfVRUUUN3ME2xNk42Ojl3IN88US=> MmfFV2FPT0WU
CAKI-1 NEfQbWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXKTWM2OD1zMj63PVEh|ryP M3LqTnNCVkeHUh?=
LXF-289 MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rr[WlEPTB;MUOuNFg{PSEQvF2= NIDURlVUSU6JRWK=
MHH-PREB-1 NXeySIJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVz4blY3UUN3ME2xN{4zPzB2IN88US=> MX3TRW5ITVJ?
EW-16 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmm0TWM2OD1zMz6zNVg4KM7:TR?= M{H0SnNCVkeHUh?=
NCI-H82 NULKUJZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4KxT2lEPTB;MUOuOFE6PSEQvF2= M{n2THNCVkeHUh?=
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OVCAR-8 NFfF[G9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HnbmlEPTB;NEeuOlg{KM7:TR?= NG\vO49USU6JRWK=
LB2241-RCC M4fwWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPvcIQ1UUN3ME20O{44OjdizszN NHXQfZZUSU6JRWK=
NCI-H358 Ml\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPGXFJzUUN3ME20PE4yOTV{IN88US=> NEfqR5hUSU6JRWK=
PANC-08-13 NEn3PItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHsWVZkUUN3ME20PE4yQDV|IN88US=> MorKV2FPT0WU
KP-N-YN NWXLcJVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln0TWM2OD12OD6yNVAzKM7:TR?= NWPmXVhqW0GQR1XS
NCI-H1755 M17HdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR6LkK3NlYh|ryP NVzlOIpbW0GQR1XS
NCI-N87 Mnf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7pR5pKSzVyPUS4MlI6QTFizszN NHLnT|lUSU6JRWK=

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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]
+ Expand
  • 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

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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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.

FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID