PD173074

For research use only. Not for use in humans.

Licensed by Pfizer Catalog No.S1264

56 publications

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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Selleck's PD173074 has been cited by 56 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 NXHhOldMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLNRYRWUUN3ME2wMlAyOjJ3IN88US=> NIS4bZFUSU6JRWK=
KG-1 NVPnemhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33TTWlEPTB;MD6wOVEzQSEQvF2= M3zTSnNCVkeHUh?=
MFM-223 Ml[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzVTWM2OD1yLkKxOVc3KM7:TR?= MWLTRW5ITVJ?
EoL-1-cell NUDuOW56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTBwM{K5PFQh|ryP M{LiU3NCVkeHUh?=
ECC10 NUD3b2M4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwM{O4PVgh|ryP MXrTRW5ITVJ?
H-EMC-SS MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf2TWM2OD1yLkO0O|E2KM7:TR?= MUfTRW5ITVJ?
AN3-CA Mo\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwNECxN|Mh|ryP NIDLcVRUSU6JRWK=
HuO-3N1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwNUS2OVMh|ryP NH74cGhUSU6JRWK=
RT-112 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW3O|lNUUN3ME2wMlU1PzBzIN88US=> NIC3[llUSU6JRWK=
NEC8 M1zI[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwNU[yPFkh|ryP MXHTRW5ITVJ?
D-263MG Mm\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwN{GxOVkh|ryP M2nQd3NCVkeHUh?=
SW962 MlrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7Hc25CUUN3ME2wMlc5QTh6IN88US=> NX7SS5BKW0GQR1XS
BV-173 NX3nTHd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwOES2NlMh|ryP NV;MVYNKW0GQR1XS
MFE-280 M3\GOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nwdmlEPTB;MD64OVg4OiEQvF2= M1PyOnNCVkeHUh?=
HuH-7 NHTkOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HROGlEPTB;MT6yOFQ3PCEQvF2= MUHTRW5ITVJ?
RS4-11 M2XmWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXjXFRJUUN3ME2xMlM{QDh4IN88US=> MkTZV2FPT0WU
DMS-114 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO3TWM2OD1zLkO2O|M4KM7:TR?= MXnTRW5ITVJ?
MSTO-211H MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFwNEezO|gh|ryP MkOxV2FPT0WU
DU-145 NVnSbWp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;qeGlEPTB;MT61PFIyPyEQvF2= Ml\xV2FPT0WU
A172 M4n5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;tcmlEPTB;MT63NFM2PSEQvF2= MXfTRW5ITVJ?
SBC-1 NHOzfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[5U2FKSzVyPUKuNFk1KM7:TR?= NV7ad3J{W0GQR1XS
H9 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHX6b5BKSzVyPUKuNVQ{ODZizszN MmLOV2FPT0WU
NCI-SNU-1 MlmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvyXIdoUUN3ME2yMlE5Ozl2IN88US=> NUDpUIkxW0GQR1XS
NCI-H720 NYfUcYtzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPTS484UUN3ME2yMlIyOjh|IN88US=> Mm[zV2FPT0WU
HCC2218 MmPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XFT2lEPTB;Mj6zO|k{QSEQvF2= M1XxRnNCVkeHUh?=
G-401 NH\3WZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXtV|FTUUN3ME2yMlQ4OTh7IN88US=> MkWwV2FPT0WU
MPP-89 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v1VmlEPTB;Mj60PFM3PCEQvF2= NYfUOpRlW0GQR1XS
697 NGfnR2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:2TWM2OD1{Lk[1N|MyKM7:TR?= NGjidFlUSU6JRWK=
KARPAS-45 MlPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjKTWM2OD1{LkewO|Q4KM7:TR?= MYTTRW5ITVJ?
MG-63 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\h[Y5TUUN3ME2yMlk1OjZ{IN88US=> M1\wS3NCVkeHUh?=
NTERA-S-cl-D1 NFyyeoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULGW5l[UUN3ME2zMlA{PDd{IN88US=> NYHQb3ZyW0GQR1XS
G-402 MonLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnxW3ZOUUN3ME2zMlEzPzJ5IN88US=> NIG4cYVUSU6JRWK=
NKM-1 NWW4c4NYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTNwMUO1OlQh|ryP NWnsdFdrW0GQR1XS
RH-18 NWXqWJl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULVXXQ4UUN3ME2zMlE6PTl6IN88US=> NU[5UoZ2W0GQR1XS
NCI-H1092 NG\tdndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{foTmlEPTB;Mz6xPVY6KM7:TR?= NYnnOohrW0GQR1XS
RPMI-8226 NGPWbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzqR4dKSzVyPUOuNlM1PDdizszN MXLTRW5ITVJ?
GAMG M1PCfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonjTWM2OD1|LkS2OVc3KM7:TR?= MV\TRW5ITVJ?
HH NIDDcGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGX1bIVKSzVyPUOuOFc3PzZizszN NV;kWVlIW0GQR1XS
RO82-W-1 NX:wc5lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoSxTWM2OD1|LkS5PFU2KM7:TR?= NYfZ[mE5W0GQR1XS
CCRF-CEM MlzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTZXZdnUUN3ME2zMlUxPDh6IN88US=> MV7TRW5ITVJ?
NBsusSR M4m5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfyTWM2OD1|Lk[zPVY6KM7:TR?= NEPZ[5RUSU6JRWK=
CHL-1 NWXwPGNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7LdI06UUN3ME2zMlY2Pzl7IN88US=> NXHCfm5JW0GQR1XS
LK-2 M{HDXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVm1d|NtUUN3ME2zMlY4OTN|IN88US=> MUPTRW5ITVJ?
Hs-578-T MnjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\6TWM2OD1|Lk[3PFc{KM7:TR?= M{jHOXNCVkeHUh?=
CTB-1 NGK5VpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETNOFZKSzVyPUOuPFAxPTFizszN MkP1V2FPT0WU
ES5 NVKwXXFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTNwOEO2N|ch|ryP MlzEV2FPT0WU
A204 NV;BS21zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTLO3hKSzVyPUOuPVIxPzVizszN NUTKSnJEW0GQR1XS
SW780 NXvmSI1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3pSGJKSzVyPUOuPVIzPDVizszN NGrwdFVUSU6JRWK=
EW-3 M3zW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzp[odKSzVyPUOuPVg6OjNizszN M3OweHNCVkeHUh?=
A704 Mn\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zhZ2lEPTB;ND6yPFczOyEQvF2= NFP6T5NUSU6JRWK=
LU-139 M3ztNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTRwM{G1N|Qh|ryP M2ntNnNCVkeHUh?=
CAL-72 M4Th[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHhTYtKSzVyPUSuOFE4PDZizszN M2TQXHNCVkeHUh?=
D-336MG MnfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLTTWM2OD12LkS2PFE4KM7:TR?= NILCWodUSU6JRWK=
LAMA-84 M1PuPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3XOWtKSzVyPUSuOVM{OSEQvF2= MlvMV2FPT0WU
GI-ME-N M3[we2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlK3TWM2OD12LkW0PFEh|ryP NHj2U5BUSU6JRWK=
KM-H2 NUK1c2hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Hxe2lEPTB;ND61OVIzOiEQvF2= M3TOfHNCVkeHUh?=
NCI-H209 NXHtSZlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1u3bmlEPTB;ND61PFI5OyEQvF2= MXzTRW5ITVJ?
IGROV-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7Bb|JKSzVyPUSuPFcyPjhizszN NEjVW4JUSU6JRWK=
L-363 M4TGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL4ZZJKSzVyPUSuPVY3PjVizszN MX\TRW5ITVJ?
SK-MEL-3 NIW4WYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTVwMkSwOkDPxE1? Mn[2V2FPT0WU
HuO9 NW\jfXFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;CO2lEPTB;NT6zPFg1OyEQvF2= NH;nXllUSU6JRWK=
NOS-1 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofVTWM2OD13LkeyPVI4KM7:TR?= MofxV2FPT0WU
NCI-H1770 MoK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnwdItOUUN3ME21Mlk2ODN{IN88US=> M3TvZnNCVkeHUh?=
SF126 MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zkWmlEPTB;Nj6yNVQxPiEQvF2= M1rYZ3NCVkeHUh?=
ML-2 M3:3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nifWlEPTB;Nj6yOFk4PyEQvF2= MmXaV2FPT0WU
CHP-134 M1K5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHrTWM2OD14LkK1NVgzKM7:TR?= M{HjfHNCVkeHUh?=
NCI-H1355 M{DMbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHRSWxPUUN3ME22MlQyPzN|IN88US=> NWPRfYppW0GQR1XS
TE-12 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33QcWlEPTB;Nj63NlY4OSEQvF2= MXnTRW5ITVJ?
A4-Fuk MojaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;NRYZ7UUN3ME22Mlc{OTR{IN88US=> NYXYVoJHW0GQR1XS
MV-4-11 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTZwN{[2NlYh|ryP MWDTRW5ITVJ?
SK-UT-1 MnXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\QeZNKSzVyPU[uPVE4QDRizszN Moq1V2FPT0WU
J-RT3-T3-5 MmrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvFTWM2OD15LkC3O|Y1KM7:TR?= MUXTRW5ITVJ?
ME-180 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzETWM2OD15LkGwOFA1KM7:TR?= NIHvdIhUSU6JRWK=
SK-MEL-28 M{DDdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj1TWM2OD15LkO3PFE6KM7:TR?= NFju[pdUSU6JRWK=
HAL-01 M3PGRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vMTGlEPTB;Nz60PFM1OSEQvF2= MV7TRW5ITVJ?
ES8 NYG2bVNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmqwTWM2OD15Lk[5OlI3KM7:TR?= MYLTRW5ITVJ?
DB NXW5RnVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInMXG1KSzVyPUiuNVE2ODRizszN MWHTRW5ITVJ?
SK-NEP-1 NFrE[IZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPTUnhKSzVyPUiuOFgyPDlizszN NVTJRYdtW0GQR1XS
COR-L88 M{nzO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r0R2lEPTB;OD61NFk5OSEQvF2= MnfVV2FPT0WU
LB1047-RCC NWnuXo1ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHqwe3BKSzVyPUiuOVIzOTJizszN NH\y[WFUSU6JRWK=
NCI-H520 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkOyTWM2OD16Lk[yNVU4KM7:TR?= NWPmdIQ5W0GQR1XS
SW954 MmLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjVTWM2OD16Lk[5O|g3KM7:TR?= M4L3eHNCVkeHUh?=
TE-6 NE\NcVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi2TWM2OD16Lke1NVQ{KM7:TR?= MV;TRW5ITVJ?
D-283MED NULidYFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S0RmlEPTB;OT6wOlU{PCEQvF2= MWTTRW5ITVJ?
DBTRG-05MG M4fv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLCeWZKSzVyPUmuNFk3ODdizszN NV;6R5ByW0GQR1XS
NCI-H446 M4\Hb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHa[IZKSzVyPUmuNlk2OjZizszN NIHE[IRUSU6JRWK=
HOS M{Hz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TrRmlEPTB;OT6zOVE{PCEQvF2= NVHne5l7W0GQR1XS
ES4 NXTNdmp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fLWmlEPTB;OT61NFU6PSEQvF2= Mn72V2FPT0WU
EW-13 M1:1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXCTWM2OD17Lki5NFU2KM7:TR?= MVvTRW5ITVJ?
IST-MES1 M1:2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml6xTWM2OD17Lkm0OVM1KM7:TR?= M3\QWHNCVkeHUh?=
CAS-1 NF\OUGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTlwOUe2OVkh|ryP MmDMV2FPT0WU
EM-2 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjHVpdKSzVyPUGwMlE{QTNizszN NFv0TYdUSU6JRWK=
SW948 M1PKTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;NVmRKSzVyPUGwMlE5QDJizszN Mlj0V2FPT0WU
OAW-42 MmXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjwRmZKSzVyPUGwMlUzPjdizszN NYPjNlJHW0GQR1XS
BE-13 NInlfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLsWlVLUUN3ME2xNE43PTd4IN88US=> M1fZ[3NCVkeHUh?=
KU812 M1uwSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vtPGlEPTB;MUCuO|M6OSEQvF2= M2PDZnNCVkeHUh?=
SK-MEL-30 NFTiZmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHGd213UUN3ME2xNE45QTBzIN88US=> MnfTV2FPT0WU
A2780 MmXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P6ZWlEPTB;MUGuNFMxQCEQvF2= Ml;GV2FPT0WU
TGBC24TKB Ml7uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTFzLkC3N|ch|ryP MX\TRW5ITVJ?
GOTO MlrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;5TWM2OD1zMT6yNFg1KM7:TR?= M1TtVXNCVkeHUh?=
NCI-H526 NGP3d4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPTPJV{UUN3ME2xNU4{QDN5IN88US=> NFXiPIRUSU6JRWK=
BHT-101 MmDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkixTWM2OD1zMT60OFU3KM7:TR?= NGWwSGJUSU6JRWK=
NCI-H1155 M{nNeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH72elhKSzVyPUGxMlQ6PDdizszN MWDTRW5ITVJ?
MCF7 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G4PGlEPTB;MUGuOlE3PyEQvF2= MmDyV2FPT0WU
MKN45 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LaPWlEPTB;MUGuO|k6OyEQvF2= MoTtV2FPT0WU
MOLT-16 NYK0SZBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\XU|hKSzVyPUGxMlk3QTJizszN MVfTRW5ITVJ?
YH-13 MmX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe0TWM2OD1zMj6wN|Q3KM7:TR?= Mnv6V2FPT0WU
P12-ICHIKAWA MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoK1TWM2OD1zMj6zPFQ2KM7:TR?= MXHTRW5ITVJ?
GR-ST M1jWfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTF{LkWyPVUh|ryP MV\TRW5ITVJ?
CAKI-1 M4TsOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF{Lke5NUDPxE1? MV3TRW5ITVJ?
LXF-289 NUL4fJp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLRTWM2OD1zMz6wPFM2KM7:TR?= MlPQV2FPT0WU
MHH-PREB-1 NWT1XYxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HoWmlEPTB;MUOuNlcxPCEQvF2= NYXwU|NKW0GQR1XS
EW-16 Mne1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrJTWM2OD1zMz6zNVg4KM7:TR?= MmXRV2FPT0WU
NCI-H82 NGKyPFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF|LkSxPVUh|ryP NIr6R|BUSU6JRWK=
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LB2241-RCC M322Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTR5LkeyO{DPxE1? MU\TRW5ITVJ?
NCI-H358 NGHhNVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj5e5h6UUN3ME20PE4yOTV{IN88US=> NW\SeVgzW0GQR1XS
PANC-08-13 NGH2VFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PEV2lEPTB;NEiuNVg2OyEQvF2= MVzTRW5ITVJ?
KP-N-YN MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnpRo1zUUN3ME20PE4zOTB{IN88US=> NUTNXFRSW0GQR1XS
NCI-H1755 M4XhVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOxdG5sUUN3ME20PE4zPzJ4IN88US=> MX\TRW5ITVJ?
NCI-N87 MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPReGx1UUN3ME20PE4zQTlzIN88US=> MmP4V2FPT0WU

... 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
Smiles CCN(CC)CCCCNC1=NC=C2C=C(C(=NC2=N1)NC(=O)NC(C)(C)C)C3=CC(=CC(=C3)OC)OC

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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