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 54 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{TGRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTBwMEGyNlUh|ryP NHPNUG9USU6JRWK=
KG-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33zPWlEPTB;MD6wOVEzQSEQvF2= NGHDSHpUSU6JRWK=
MFM-223 M3OzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXITHFJUUN3ME2wMlIyPTd4IN88US=> MXrTRW5ITVJ?
EoL-1-cell NYHydWZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfjcpVHUUN3ME2wMlMzQTh2IN88US=> M{nlRXNCVkeHUh?=
ECC10 NH7heoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3TWpdKSzVyPUCuN|M5QThizszN NFy1S5BUSU6JRWK=
H-EMC-SS M1Xzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\BTWM2OD1yLkO0O|E2KM7:TR?= MX;TRW5ITVJ?
AN3-CA NXjuXZRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjvRY9KSzVyPUCuOFAyOzNizszN NGf6[21USU6JRWK=
HuO-3N1 Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwNUS2OVMh|ryP M173SHNCVkeHUh?=
RT-112 NV32NYN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfyTWM2OD1yLkW0O|AyKM7:TR?= M4\EUXNCVkeHUh?=
NEC8 M4TjSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7yTWM2OD1yLkW2Nlg6KM7:TR?= NHi5cWpUSU6JRWK=
D-263MG M2XGRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr0TWM2OD1yLkexNVU6KM7:TR?= MlzXV2FPT0WU
SW962 M3f3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LIWWlEPTB;MD63PFk5QCEQvF2= Mki5V2FPT0WU
BV-173 NFHqVHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnLTWM2OD1yLki0OlI{KM7:TR?= M4\JcXNCVkeHUh?=
MFE-280 NHS1TXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fZfWlEPTB;MD64OVg4OiEQvF2= M13rRnNCVkeHUh?=
HuH-7 Ml3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTFwMkS0OlQh|ryP Ml\uV2FPT0WU
RS4-11 M4r6bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3uNoxKSzVyPUGuN|M5QDZizszN MYfTRW5ITVJ?
DMS-114 NYPuOVJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\Jc5ZKSzVyPUGuN|Y4OzdizszN MoLNV2FPT0WU
MSTO-211H NFjJXGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO4TWM2OD1zLkS3N|c5KM7:TR?= MX3TRW5ITVJ?
DU-145 NV;EVHhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HrXGlEPTB;MT61PFIyPyEQvF2= MnzQV2FPT0WU
A172 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXjbZlNUUN3ME2xMlcxOzV3IN88US=> M2rtb3NCVkeHUh?=
SBC-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1O2VGlEPTB;Mj6wPVQh|ryP MWDTRW5ITVJ?
H9 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnSbnJMUUN3ME2yMlE1OzB4IN88US=> Ml7UV2FPT0WU
NCI-SNU-1 M{HHdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzJN|NzUUN3ME2yMlE5Ozl2IN88US=> Mny3V2FPT0WU
NCI-H720 NEP5SJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXETWM2OD1{LkKxNlg{KM7:TR?= NYPWOmFKW0GQR1XS
HCC2218 NGD5bIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJwM{e5N|kh|ryP M2\zNnNCVkeHUh?=
G-401 NI\1PJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFm1OVFKSzVyPUKuOFcyQDlizszN NIrS[IxUSU6JRWK=
MPP-89 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTJwNEizOlQh|ryP NFXFTYFUSU6JRWK=
697 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH6wXmJKSzVyPUKuOlU{OzFizszN NXfKTlIyW0GQR1XS
KARPAS-45 MkPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\0TWM2OD1{LkewO|Q4KM7:TR?= NGmze2lUSU6JRWK=
MG-63 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXTTpRKSzVyPUKuPVQzPjJizszN M{C4[nNCVkeHUh?=
NTERA-S-cl-D1 M1XsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTRTWM2OD1|LkCzOFczKM7:TR?= NFL0fWdUSU6JRWK=
G-402 M{H0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX32RndkUUN3ME2zMlEzPzJ5IN88US=> NHSxVZNUSU6JRWK=
NKM-1 M1SxeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljwTWM2OD1|LkGzOVY1KM7:TR?= Mn\2V2FPT0WU
RH-18 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTNwMUm1PVgh|ryP M1;5[3NCVkeHUh?=
NCI-H1092 M33FWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmCwTWM2OD1|LkG5Olkh|ryP M2n1[HNCVkeHUh?=
RPMI-8226 M2TIPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNwMkO0OFch|ryP Mon5V2FPT0WU
GAMG M4rVPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLlRWZOUUN3ME2zMlQ3PTd4IN88US=> M13MR3NCVkeHUh?=
HH M1W5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2KxZWlEPTB;Mz60O|Y4PiEQvF2= NXH2S|BvW0GQR1XS
RO82-W-1 NYP5S4JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1OzSWlEPTB;Mz60PVg2PSEQvF2= NEHobmdUSU6JRWK=
CCRF-CEM NXvyZ5Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;lTWM2OD1|LkWwOFg5KM7:TR?= NVLWRYx3W0GQR1XS
NBsusSR MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLGWmhKSzVyPUOuOlM6PjlizszN NFPV[HVUSU6JRWK=
CHL-1 M2LOeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTNwNkW3PVkh|ryP NH:5[WRUSU6JRWK=
LK-2 NEeyT|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTNwNkexN|Mh|ryP MVvTRW5ITVJ?
Hs-578-T NFT2cmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;KNmlEPTB;Mz62O|g4OyEQvF2= M4m2UnNCVkeHUh?=
CTB-1 NHrVT2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn1TWM2OD1|LkiwNFUyKM7:TR?= MVrTRW5ITVJ?
ES5 MkWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTNwOEO2N|ch|ryP MUfTRW5ITVJ?
A204 NHHHd5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDvU3FKSzVyPUOuPVIxPzVizszN NE\nOotUSU6JRWK=
SW780 NYnvfG02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjaTWM2OD1|LkmyNlQ2KM7:TR?= MVHTRW5ITVJ?
EW-3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\zNWlEPTB;Mz65PFkzOyEQvF2= M1vrfXNCVkeHUh?=
A704 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjyeZVUUUN3ME20MlI5PzJ|IN88US=> MVHTRW5ITVJ?
LU-139 NHPFd21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP3TWM2OD12LkOxOVM1KM7:TR?= NIrGepBUSU6JRWK=
CAL-72 NHPrfHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1[wdWlEPTB;ND60NVc1PiEQvF2= NFvTN4hUSU6JRWK=
D-336MG NGXuO4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX70WY9oUUN3ME20MlQ3QDF5IN88US=> NVvwcItzW0GQR1XS
LAMA-84 NIXDTFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u3bmlEPTB;ND61N|MyKM7:TR?= MYHTRW5ITVJ?
GI-ME-N NWHwb5h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr5N5BKUUN3ME20MlU1QDFizszN NFvhV3ZUSU6JRWK=
KM-H2 NW\TRWlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH35XWFKSzVyPUSuOVUzOjJizszN NG\XdZhUSU6JRWK=
NCI-H209 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTRwNUiyPFMh|ryP NE\0Z|NUSU6JRWK=
IGROV-1 NInaSWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH3TWM2OD12Lki3NVY5KM7:TR?= MXPTRW5ITVJ?
L-363 NWq2OVVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDtU2RKSzVyPUSuPVY3PjVizszN NILNN3RUSU6JRWK=
SK-MEL-3 NU\aW5VbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTKXlRoUUN3ME21MlI1ODZizszN MX;TRW5ITVJ?
HuO9 M2fDNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fqSGlEPTB;NT6zPFg1OyEQvF2= M4DWUHNCVkeHUh?=
NOS-1 NEDRSmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jwfmlEPTB;NT63NlkzPyEQvF2= MmjDV2FPT0WU
NCI-H1770 NEj0R4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;VdWlEPTB;NT65OVA{OiEQvF2= MnO4V2FPT0WU
SF126 MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTZwMkG0NFYh|ryP NVzYbm9bW0GQR1XS
ML-2 M2i5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTBNpJmUUN3ME22MlI1QTd5IN88US=> NH\zWYZUSU6JRWK=
CHP-134 NHHSZohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nHO2lEPTB;Nj6yOVE5OiEQvF2= MXvTRW5ITVJ?
NCI-H1355 MkHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\hRpNkUUN3ME22MlQyPzN|IN88US=> NELy[VlUSU6JRWK=
TE-12 NH:yfGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XGcWlEPTB;Nj63NlY4OSEQvF2= NEXxT2NUSU6JRWK=
A4-Fuk NUHXb5VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fyOGlEPTB;Nj63N|E1OiEQvF2= M37l[HNCVkeHUh?=
MV-4-11 NWra[ottT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPvOZJKSzVyPU[uO|Y3OjZizszN NVzpTVRSW0GQR1XS
SK-UT-1 NW\qTJM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfSZWhnUUN3ME22MlkyPzh2IN88US=> NET6VXVUSU6JRWK=
J-RT3-T3-5 M3fWNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTdwMEe3OlQh|ryP MVvTRW5ITVJ?
ME-180 NF;hV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTCTWM2OD15LkGwOFA1KM7:TR?= NHH5SVZUSU6JRWK=
SK-MEL-28 M3f1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTdwM{e4NVkh|ryP MmW3V2FPT0WU
HAL-01 MkWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfHTWM2OD15LkS4N|QyKM7:TR?= MmjiV2FPT0WU
ES8 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTdwNkm2NlYh|ryP NGrSVWxUSU6JRWK=
DB NX;X[GV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfFTWM2OD16LkGxOVA1KM7:TR?= M{DGbnNCVkeHUh?=
SK-NEP-1 NUP5OXE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRThwNEixOFkh|ryP NEXaOXdUSU6JRWK=
COR-L88 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDGTWM2OD16LkWwPVgyKM7:TR?= Mn21V2FPT0WU
LB1047-RCC MljpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TJWmlEPTB;OD61NlIyOiEQvF2= NVzvTXVrW0GQR1XS
NCI-H520 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRThwNkKxOVch|ryP M4W0bHNCVkeHUh?=
SW954 Mn\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HsW2lEPTB;OD62PVc5PiEQvF2= NXHETmgzW0GQR1XS
TE-6 NXzqZ3VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\TVWJFUUN3ME24Mlc2OTR|IN88US=> MXXTRW5ITVJ?
D-283MED M3TzNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfRdo0{UUN3ME25MlA3PTN2IN88US=> NV\GZZFTW0GQR1XS
DBTRG-05MG NWPrTIV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTlwMEm2NFch|ryP M17MfnNCVkeHUh?=
NCI-H446 MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkixTWM2OD17LkK5OVI3KM7:TR?= NUnDZVd3W0GQR1XS
HOS NWDVR3pXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LJVmlEPTB;OT6zOVE{PCEQvF2= NVHIZoh1W0GQR1XS
ES4 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC0O4VKSzVyPUmuOVA2QTVizszN NHzXUJNUSU6JRWK=
EW-13 MlvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTVZ2cyUUN3ME25Mlg6ODV3IN88US=> M1vlNXNCVkeHUh?=
IST-MES1 M1;CSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTlwOUS1N|Qh|ryP MoH1V2FPT0WU
CAS-1 M4HmUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjHTWM2OD17Lkm3OlU6KM7:TR?= M{\NRXNCVkeHUh?=
EM-2 M2LnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrjPZZKSzVyPUGwMlE{QTNizszN Ml7uV2FPT0WU
SW948 MoOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTFyLkG4PFIh|ryP NVLkUIhoW0GQR1XS
OAW-42 M{D4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfmTWM2OD1zMD61NlY4KM7:TR?= M3j2SnNCVkeHUh?=
BE-13 NH6xOHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFyLk[1O|Yh|ryP NV\w[mhlW0GQR1XS
KU812 NEXtcY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXOzOoJyUUN3ME2xNE44OzlzIN88US=> M13Xb3NCVkeHUh?=
SK-MEL-30 MlnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFyLki5NFEh|ryP MW\TRW5ITVJ?
A2780 NIXqW4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPJPW9kUUN3ME2xNU4xOzB6IN88US=> NYrFVG9JW0GQR1XS
TGBC24TKB M1vMfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS0U|cxUUN3ME2xNU4xPzN5IN88US=> NV7TNFlkW0GQR1XS
GOTO MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HEO2lEPTB;MUGuNlA5PCEQvF2= MUHTRW5ITVJ?
NCI-H526 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;SZYdKSzVyPUGxMlM5OzdizszN NWPObI5jW0GQR1XS
BHT-101 NV\nbYFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrBNnpuUUN3ME2xNU41PDV4IN88US=> NYjvN3plW0GQR1XS
NCI-H1155 NYrwXndlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fhT2lEPTB;MUGuOFk1PyEQvF2= NYLncmZsW0GQR1XS
MCF7 NYHYdlE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTFzLk[xOlch|ryP NXjXV2FEW0GQR1XS
MKN45 NV:2cIt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTFzLke5PVMh|ryP MVjTRW5ITVJ?
MOLT-16 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPNdWc2UUN3ME2xNU46Pjl{IN88US=> M1S2S3NCVkeHUh?=
YH-13 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF{LkCzOFYh|ryP NG\mcIdUSU6JRWK=
P12-ICHIKAWA MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTF{LkO4OFUh|ryP MYrTRW5ITVJ?
GR-ST NFnkeFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknkTWM2OD1zMj61Nlk2KM7:TR?= MYfTRW5ITVJ?
CAKI-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vLbWlEPTB;MUKuO|kyKM7:TR?= MYTTRW5ITVJ?
LXF-289 NVnGflNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTF|LkC4N|Uh|ryP M3\GeXNCVkeHUh?=
MHH-PREB-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHjTopKSzVyPUGzMlI4ODRizszN NF\rOnNUSU6JRWK=
EW-16 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHad4hXUUN3ME2xN{4{OTh5IN88US=> M{m5cnNCVkeHUh?=
NCI-H82 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTF|LkSxPVUh|ryP MmG2V2FPT0WU
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LB2241-RCC NF[5bYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\KW2lEPTB;NEeuO|I4KM7:TR?= MWjTRW5ITVJ?
NCI-H358 NV;QS2pNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTR6LkGxOVIh|ryP NYrjSpBGW0GQR1XS
PANC-08-13 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3mz[2lEPTB;NEiuNVg2OyEQvF2= NGDxXXlUSU6JRWK=
KP-N-YN NHPPV49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3iSm1KSzVyPUS4MlIyODJizszN M{LySXNCVkeHUh?=
NCI-H1755 Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTR6LkK3NlYh|ryP MYrTRW5ITVJ?
NCI-N87 NF:wb2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XPOGlEPTB;NEiuNlk6OSEQvF2= NHvqS2hUSU6JRWK=

... 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