PD173074

For research use only.

Licensed by Pfizer Catalog No.S1264

71 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. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

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Selleck's PD173074 has been cited by 71 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. 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

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 M1LK[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HvTmlEPTB;MD6wNVIzPSEQvF2= M1vwfnNCVkeHUh?=
KG-1 NVTYS2hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj0TWM2OD1yLkC1NVI6KM7:TR?= M{W0ZXNCVkeHUh?=
MFM-223 NFKwV5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPk[|JKSzVyPUCuNlE2PzZizszN MWTTRW5ITVJ?
EoL-1-cell NVPHZZVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Tj[WlEPTB;MD6zNlk5PCEQvF2= NF;ZcFBUSU6JRWK=
ECC10 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz3SXVKSzVyPUCuN|M5QThizszN NECxOW5USU6JRWK=
H-EMC-SS NWfTXWJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofhTWM2OD1yLkO0O|E2KM7:TR?= NHX1dppUSU6JRWK=
AN3-CA NIj1PYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVi4bIF6UUN3ME2wMlQxOTN|IN88US=> NYPqPVBFW0GQR1XS
HuO-3N1 NWPYfoxZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTITWM2OD1yLkW0OlU{KM7:TR?= MXPTRW5ITVJ?
RT-112 M1TVOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHnSYtiUUN3ME2wMlU1PzBzIN88US=> NFjWbnRUSU6JRWK=
NEC8 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPyOlM6UUN3ME2wMlU3Ojh7IN88US=> NUnr[lRkW0GQR1XS
D-263MG M2nSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37qTmlEPTB;MD63NVE2QSEQvF2= M4TTcHNCVkeHUh?=
SW962 M2\FSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NESxVIVKSzVyPUCuO|g6QDhizszN MY\TRW5ITVJ?
BV-173 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFezRoxKSzVyPUCuPFQ3OjNizszN MkT4V2FPT0WU
MFE-280 NUnk[JZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwOEW4O|Ih|ryP M3\GfHNCVkeHUh?=
HuH-7 M1PNPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHpTWM2OD1zLkK0OFY1KM7:TR?= MUPTRW5ITVJ?
RS4-11 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTCboJKSzVyPUGuN|M5QDZizszN NXLxb|NoW0GQR1XS
DMS-114 NIn1O|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfkVVlYUUN3ME2xMlM3PzN5IN88US=> MoGxV2FPT0WU
MSTO-211H M2X2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3nTWM2OD1zLkS3N|c5KM7:TR?= M4i2WnNCVkeHUh?=
DU-145 M2Txb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\VTWM2OD1zLkW4NlE4KM7:TR?= M133cHNCVkeHUh?=
A172 NVu4eZdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFwN{CzOVUh|ryP NYTmTnlJW0GQR1XS
SBC-1 NX;1Z|F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTJwMEm0JO69VQ>? NGP4TYxUSU6JRWK=
H9 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXv5TFB5UUN3ME2yMlE1OzB4IN88US=> NG\R[25USU6JRWK=
NCI-SNU-1 NX\ZdpVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XNfWlEPTB;Mj6xPFM6PCEQvF2= Mom5V2FPT0WU
NCI-H720 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJwMkGyPFMh|ryP MUHTRW5ITVJ?
HCC2218 MlS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJwM{e5N|kh|ryP MmrEV2FPT0WU
G-401 Ml\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7wXlk5UUN3ME2yMlQ4OTh7IN88US=> NFPm[5VUSU6JRWK=
MPP-89 NHnVcWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzHS2VKSzVyPUKuOFg{PjRizszN M4rCeXNCVkeHUh?=
697 NYLnWWxbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTZPIRCUUN3ME2yMlY2OzNzIN88US=> M{fCVHNCVkeHUh?=
KARPAS-45 Ml;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjBS4hKSzVyPUKuO|A4PDdizszN NEn0O2VUSU6JRWK=
MG-63 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTJwOUSyOlIh|ryP M1fzT3NCVkeHUh?=
NTERA-S-cl-D1 NGezRmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTNwMEO0O|Ih|ryP M4r5WXNCVkeHUh?=
G-402 NWTFNW9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3YbJE6UUN3ME2zMlEzPzJ5IN88US=> NGm1e2hUSU6JRWK=
NKM-1 NX[zUI45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWGx[3lyUUN3ME2zMlE{PTZ2IN88US=> M1XZbHNCVkeHUh?=
RH-18 M{G5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXJ[25UUUN3ME2zMlE6PTl6IN88US=> NV7QTGQzW0GQR1XS
NCI-H1092 M{fzbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTNwMUm2PUDPxE1? NVLWfpZtW0GQR1XS
RPMI-8226 NH:0[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTNwMkO0OFch|ryP Mn\mV2FPT0WU
GAMG MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTNwNE[1O|Yh|ryP M{LmT3NCVkeHUh?=
HH MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojaTWM2OD1|LkS3Olc3KM7:TR?= NGPHfmdUSU6JRWK=
RO82-W-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjUTWM2OD1|LkS5PFU2KM7:TR?= NVK3PGFQW0GQR1XS
CCRF-CEM MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj4WXJKSzVyPUOuOVA1QDhizszN MmO5V2FPT0WU
NBsusSR MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTNwNkO5Olkh|ryP M1TBRXNCVkeHUh?=
CHL-1 M4T6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rzTmlEPTB;Mz62OVc6QSEQvF2= M{HzWnNCVkeHUh?=
LK-2 NVTDUXJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfIbIxKSzVyPUOuOlcyOzNizszN M2L2[XNCVkeHUh?=
Hs-578-T M{LRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTNwNke4O|Mh|ryP MYPTRW5ITVJ?
CTB-1 NIXCdHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjvUIltUUN3ME2zMlgxODVzIN88US=> M3vhPHNCVkeHUh?=
ES5 MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\LV2lEPTB;Mz64N|Y{PyEQvF2= NHTGenRUSU6JRWK=
A204 M3fufmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17STmlEPTB;Mz65NlA4PSEQvF2= MmHSV2FPT0WU
SW780 M{jvSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHzdWdvUUN3ME2zMlkzOjR3IN88US=> Mn[yV2FPT0WU
EW-3 MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq1eW93UUN3ME2zMlk5QTJ|IN88US=> NWPkS41kW0GQR1XS
A704 Mn22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTRwMki3NlMh|ryP M4Xa[nNCVkeHUh?=
LU-139 NWLK[YZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTMTWM2OD12LkOxOVM1KM7:TR?= MmrDV2FPT0WU
CAL-72 M3uzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jJO2lEPTB;ND60NVc1PiEQvF2= NF7QZ5NUSU6JRWK=
D-336MG NU\KWXlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml2zTWM2OD12LkS2PFE4KM7:TR?= MWLTRW5ITVJ?
LAMA-84 MmPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnTdnNKSzVyPUSuOVM{OSEQvF2= NWL5V5QxW0GQR1XS
GI-ME-N NFvjNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTRwNUS4NUDPxE1? NUjZWIxtW0GQR1XS
KM-H2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzoWWpKSzVyPUSuOVUzOjJizszN NE\wd2VUSU6JRWK=
NCI-H209 MoHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzU[nZKSzVyPUSuOVgzQDNizszN NGDRTJVUSU6JRWK=
IGROV-1 NGjtVZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTRwOEexOlgh|ryP MmC1V2FPT0WU
L-363 M2fH[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HQd2lEPTB;ND65OlY3PSEQvF2= NWH2eXVOW0GQR1XS
SK-MEL-3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;YTWM2OD13LkK0NFYh|ryP NIDmVHBUSU6JRWK=
HuO9 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\ydpRKSzVyPUWuN|g5PDNizszN MU\TRW5ITVJ?
NOS-1 NXXZbWpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\lV4xKSzVyPUWuO|I6OjdizszN M33WWXNCVkeHUh?=
NCI-H1770 NFPPcVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTVwOUWwN|Ih|ryP MWXTRW5ITVJ?
SF126 NHLF[3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTGN4RKSzVyPU[uNlE1ODZizszN NFHJU|hUSU6JRWK=
ML-2 NWnINFJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fKd2lEPTB;Nj6yOFk4PyEQvF2= NEHmWmNUSU6JRWK=
CHP-134 M1XycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoqzTWM2OD14LkK1NVgzKM7:TR?= MUTTRW5ITVJ?
NCI-H1355 M4nZWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPJOGRKSzVyPU[uOFE4OzNizszN MnjEV2FPT0WU
TE-12 MmDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPQTWM2OD14LkeyOlcyKM7:TR?= NI\zT3JUSU6JRWK=
A4-Fuk NICzS5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HzfmlEPTB;Nj63N|E1OiEQvF2= MX\TRW5ITVJ?
MV-4-11 M{nNRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTZwN{[2NlYh|ryP NHjSTmJUSU6JRWK=
SK-UT-1 M3Xv[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTZwOUG3PFQh|ryP NFfpSFBUSU6JRWK=
J-RT3-T3-5 MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTdwMEe3OlQh|ryP M1HBdXNCVkeHUh?=
ME-180 NIHXWFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGWxNGFKSzVyPUeuNVA1ODRizszN NI\RO4FUSU6JRWK=
SK-MEL-28 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\ZN2lEPTB;Nz6zO|gyQSEQvF2= NF\rVnRUSU6JRWK=
HAL-01 NGfZbIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTdwNEizOFEh|ryP NWXjUHZXW0GQR1XS
ES8 NGrZ[JlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELyXoVKSzVyPUeuOlk3OjZizszN M3SzbHNCVkeHUh?=
DB NXL4NWFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRThwMUG1NFQh|ryP MUTTRW5ITVJ?
SK-NEP-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjLUVZKSzVyPUiuOFgyPDlizszN MWXTRW5ITVJ?
COR-L88 NFTvR|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLQN|lKSzVyPUiuOVA6QDFizszN MX\TRW5ITVJ?
LB1047-RCC NI\TOYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFW5bnpKSzVyPUiuOVIzOTJizszN NYq4RWdEW0GQR1XS
NCI-H520 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz2TWM2OD16Lk[yNVU4KM7:TR?= M1fy[3NCVkeHUh?=
SW954 NH;rVpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrlW|hKSzVyPUiuOlk4QDZizszN NH6zb|VUSU6JRWK=
TE-6 M{LFXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRThwN{WxOFMh|ryP NILhVmxUSU6JRWK=
D-283MED NHzhW5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHwTWM2OD17LkC2OVM1KM7:TR?= NETaTWlUSU6JRWK=
DBTRG-05MG NGH3V4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnkTWM2OD17LkC5OlA4KM7:TR?= NEP2T3ZUSU6JRWK=
NCI-H446 NInsO25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnpTWM2OD17LkK5OVI3KM7:TR?= NWDmb4ptW0GQR1XS
HOS NEPveFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTlwM{WxN|Qh|ryP NYPaTIlVW0GQR1XS
ES4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDNS2NKSzVyPUmuOVA2QTVizszN MUfTRW5ITVJ?
EW-13 NFnmbYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTlwOEmwOVUh|ryP MXXTRW5ITVJ?
IST-MES1 MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{j2T2lEPTB;OT65OFU{PCEQvF2= NWTkdpV2W0GQR1XS
CAS-1 MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\IPYlKSzVyPUmuPVc3PTlizszN Mn\PV2FPT0WU
EM-2 MmHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnrdHMxUUN3ME2xNE4yOzl|IN88US=> Mn3OV2FPT0WU
SW948 M3rNNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmW0TWM2OD1zMD6xPFgzKM7:TR?= NUPWPZo2W0GQR1XS
OAW-42 NWnDVpdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LrZWlEPTB;MUCuOVI3PyEQvF2= M4j5ZXNCVkeHUh?=
BE-13 MlXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYThS2ptUUN3ME2xNE43PTd4IN88US=> Mlr4V2FPT0WU
KU812 M1rLfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L0c2lEPTB;MUCuO|M6OSEQvF2= MnrsV2FPT0WU
SK-MEL-30 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH5XIUyUUN3ME2xNE45QTBzIN88US=> NH7o[|dUSU6JRWK=
A2780 NH7WO3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFzLkCzNFgh|ryP NYDIO4g3W0GQR1XS
TGBC24TKB NWfXXoxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvDTWM2OD1zMT6wO|M4KM7:TR?= NF;vdoNUSU6JRWK=
GOTO M1\kd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTFzLkKwPFQh|ryP Mn;5V2FPT0WU
NCI-H526 MnGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjsZ5BKSzVyPUGxMlM5OzdizszN MUTTRW5ITVJ?
BHT-101 NGTDTIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HWUGlEPTB;MUGuOFQ2PiEQvF2= NIPSR|dUSU6JRWK=
NCI-H1155 M3L2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPkfWUxUUN3ME2xNU41QTR5IN88US=> MYLTRW5ITVJ?
MCF7 M4nZUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXNR5pKSzVyPUGxMlYyPjdizszN NYGwU2F1W0GQR1XS
MKN45 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\DbWlEPTB;MUGuO|k6OyEQvF2= MV7TRW5ITVJ?
MOLT-16 NETRToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Gye2lEPTB;MUGuPVY6OiEQvF2= NYLjSWVnW0GQR1XS
YH-13 M3X6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zFS2lEPTB;MUKuNFM1PiEQvF2= NV3iRlV6W0GQR1XS
P12-ICHIKAWA NXHue4VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTF{LkO4OFUh|ryP NUPDPVdqW0GQR1XS
GR-ST M4f1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqxTWM2OD1zMj61Nlk2KM7:TR?= Mk\xV2FPT0WU
CAKI-1 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\hTWM2OD1zMj63PVEh|ryP NEni[XdUSU6JRWK=
LXF-289 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;OTWM2OD1zMz6wPFM2KM7:TR?= Ml;GV2FPT0WU
MHH-PREB-1 MnTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX2TWM2OD1zMz6yO|A1KM7:TR?= NEjSVnNUSU6JRWK=
EW-16 NXyxbnRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTRbHBKSzVyPUGzMlMyQDdizszN M4rlcHNCVkeHUh?=
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T98G NYDkZWEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTR5LkW0O{DPxE1? NFzWV5hUSU6JRWK=
OVCAR-8 NUm2SnNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\BTWM2OD12Nz62PFMh|ryP NGXpSWFUSU6JRWK=
LB2241-RCC NXXrSXNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljyTWM2OD12Nz63Nlch|ryP NEPW[WJUSU6JRWK=
NCI-H358 NHTpPXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFv3dlZKSzVyPUS4MlEyPTJizszN NUj0Um9VW0GQR1XS
PANC-08-13 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLjTWM2OD12OD6xPFU{KM7:TR?= M1WxeHNCVkeHUh?=
KP-N-YN MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonaTWM2OD12OD6yNVAzKM7:TR?= MkP3V2FPT0WU
NCI-H1755 Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTR6LkK3NlYh|ryP NWflS5FVW0GQR1XS
NCI-N87 Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rITmlEPTB;NEiuNlk6OSEQvF2= MUnTRW5ITVJ?

... 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
  • Dosages: ~2 mg/kg/day
  • Administration: Administered intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (190.95 mM)
Water Insoluble
Ethanol '100 mg/mL
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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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:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Mass Concentration Volume Molecular Weight

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