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.

Size Price Stock Quantity  
In DMSO USD 98 In stock
USD 70 In stock
USD 120 In stock
USD 470 In stock
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7 Customer Reviews

  • The inhibitor PD173074 (A) or PD184352 (B) was administered to one uterine horn of Hand2d/d mice on day 3 of pregnancy (n = 5). The other horn served as vehicle-treated control. Uterine horns were collected on the morning of day 4, and sections were subjected to IHC to detect p-FRS2, p-ERK1/2, and Ki-67. (C) IHC of pERa and Muc-1 in uterine sections of Hand2d/d mice treated with PD173074 or PD184352.

    Science 2011 331(6019), 912-6. PD173074 purchased from Selleck.

    Inhibition of FGFR signaling pathway by FGFR inhibitor PD173074 in mouse xenograft tumors. Bladder cancer SW780 cells were implanted in mice and treated with PD173074 after tumor formation as shown in B. Protein lysates of tumor tissues were prepared and immunoblotted with antibodies against phospho-ERK1/2, pan-ERK1/2, and γ-tubulin.

    Cancer Discov 2013 3(6), 636-47. PD173074 purchased from Selleck.

  • FGFR inhibitors block signaling in FGFR2-fusion-expressing cells. Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIH3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 uM BGJ398, and 0.2 and 1 uM PD173074 were immunoblotted with the relevant antibodies. β-Actin was used as a loading control.

    Hepatology 2014 59(4) ,1427-34. PD173074 purchased from Selleck.

    The level of p-FRS2 was examined in the uterine sections of Msx1f/fMsx2f/f (upper panel) and Msx1d/dMsx2d/d (lower panel) mice on day 4 of pregnancy by immunohistochemistry. Magnification: a and d: 10 x, b and e: 20 x, c and f: 40x. FGFR-specific inhibitor PD173074 was applied to one uterine horn of Msx1d/dMsx2d/d (n = 3) mice on day 3 of pregnancy. The other horn served as vehicle-treated control. Uterine horns were collected on day 4 morning and sections were subjected to immunohistochemistry to detect p-FRS2, Ki67, and Muc-1.

    PLoS Genet 2012 8(2), e1002500. PD173074 purchased from Selleck.

  • Cells were incubated with DMSO control, 10 uM TGFBR inhibitor or 10 uM FGFR inhibitor PD173074 for 1 h. Cells were fixed, labeled with anti-GM130 (red) and analyzed by confocal microscopy. Images were analyzed using Image J (n = 3 experiments, >100 cells per condition). Scale bars, 10 uM.

    J Cell Sci 2014 10.1242/jcs.159608. PD173074 purchased from Selleck.

    Effects of antagonists for RAGE (FPS-ZM), TLR-4 (TAK-242) and FGFR1 (PD and BGJ) on the S100B-induced alterations in glucose metabolism in L6 cells treated for 6 h. (A) Effects of FPS-ZM, (B) TAK-242 and (C) PD and BGJ on the S100B inhibition of glucose consumption.

    Am J Physiol Endocrinol Metab, 2017, 312(6):E471-E481. PD173074 purchased from Selleck.

  • Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 ℃ for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle- alone control, 27℃ represents temperature rescue of F508-CFTR at 27℃, 37℃ represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity.

    Biochem Bioph Res Co 2012 11(9), 745-57. PD173074 purchased from Selleck.

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 M2HuOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwMEGyNlUh|ryP M1\obnNCVkeHUh?=
KG-1 NUH5c3NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHIT2pKSzVyPUCuNFUyOjlizszN MV\TRW5ITVJ?
MFM-223 NF;6PFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\VNI1KSzVyPUCuNlE2PzZizszN MVTTRW5ITVJ?
EoL-1-cell NULYfJZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Ozd2lEPTB;MD6zNlk5PCEQvF2= Ml2wV2FPT0WU
ECC10 MnW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f4SmlEPTB;MD6zN|g6QCEQvF2= M1PkXHNCVkeHUh?=
H-EMC-SS NXSxR21iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP2TWM2OD1yLkO0O|E2KM7:TR?= MkD5V2FPT0WU
AN3-CA MlL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\ucWlEPTB;MD60NFE{OyEQvF2= NIO0[ndUSU6JRWK=
HuO-3N1 M4PW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLRTWM2OD1yLkW0OlU{KM7:TR?= NUPPbVlmW0GQR1XS
RT-112 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PHTmlEPTB;MD61OFcxOSEQvF2= MkLIV2FPT0WU
NEC8 MlvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTFTWM2OD1yLkW2Nlg6KM7:TR?= MYXTRW5ITVJ?
D-263MG NVHMbFY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwN{GxOVkh|ryP MoXPV2FPT0WU
SW962 MnroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[2TWM2OD1yLke4PVg5KM7:TR?= Mn7EV2FPT0WU
BV-173 NULtZ5RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkKwTWM2OD1yLki0OlI{KM7:TR?= M2XrV3NCVkeHUh?=
MFE-280 NUHxeGc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDmfo5VUUN3ME2wMlg2QDd{IN88US=> MUHTRW5ITVJ?
HuH-7 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIm3UFNKSzVyPUGuNlQ1PjRizszN NVjHXmhjW0GQR1XS
RS4-11 NVTFcZZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2m4TGlEPTB;MT6zN|g5PiEQvF2= NH;4enJUSU6JRWK=
DMS-114 M3X2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LDRmlEPTB;MT6zOlc{PyEQvF2= MXzTRW5ITVJ?
MSTO-211H MkLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFwNEezO|gh|ryP M2O5OHNCVkeHUh?=
DU-145 NILzN4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\5[GNSUUN3ME2xMlU5OjF5IN88US=> NUH0WmhLW0GQR1XS
A172 NFnKT4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTFwN{CzOVUh|ryP M{HlNHNCVkeHUh?=
SBC-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HVfmlEPTB;Mj6wPVQh|ryP NVzVcFk5W0GQR1XS
H9 M4\uZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJwMUSzNFYh|ryP M2rX[nNCVkeHUh?=
NCI-SNU-1 M1vsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TjVmlEPTB;Mj6xPFM6PCEQvF2= MoD5V2FPT0WU
NCI-H720 MkTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi1R417UUN3ME2yMlIyOjh|IN88US=> M4HvR3NCVkeHUh?=
HCC2218 M{X5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XrSWlEPTB;Mj6zO|k{QSEQvF2= Mne0V2FPT0WU
G-401 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTJwNEexPFkh|ryP MUHTRW5ITVJ?
MPP-89 NYPvVVN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojWTWM2OD1{LkS4N|Y1KM7:TR?= NHraVHFUSU6JRWK=
697 M4DPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTKTWM2OD1{Lk[1N|MyKM7:TR?= MoD5V2FPT0WU
KARPAS-45 M{KyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHJW2NYUUN3ME2yMlcxPzR5IN88US=> MmfQV2FPT0WU
MG-63 NGK0fJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XaRmlEPTB;Mj65OFI3OiEQvF2= NGnMSIVUSU6JRWK=
NTERA-S-cl-D1 NFvKd5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;kbWlEPTB;Mz6wN|Q4OiEQvF2= M2\xWXNCVkeHUh?=
G-402 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zyWGlEPTB;Mz6xNlczPyEQvF2= M3LUZ3NCVkeHUh?=
NKM-1 NXe3[nJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HJT2lEPTB;Mz6xN|U3PCEQvF2= NGGxe5lUSU6JRWK=
RH-18 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP4TWM2OD1|LkG5OVk5KM7:TR?= MUHTRW5ITVJ?
NCI-H1092 NUf1fW5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13oRWlEPTB;Mz6xPVY6KM7:TR?= MlfhV2FPT0WU
RPMI-8226 Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7OTWM2OD1|LkKzOFQ4KM7:TR?= NFjWPWhUSU6JRWK=
GAMG Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\wR2lEPTB;Mz60OlU4PiEQvF2= MX7TRW5ITVJ?
HH NFG4UIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\ZTWM2OD1|LkS3Olc3KM7:TR?= NH;6[WNUSU6JRWK=
RO82-W-1 NX7hVWFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFWzUJRKSzVyPUOuOFk5PTVizszN NXvHdmU{W0GQR1XS
CCRF-CEM NX\tZZZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3DTWM2OD1|LkWwOFg5KM7:TR?= MWnTRW5ITVJ?
NBsusSR MnfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vDfmlEPTB;Mz62N|k3QSEQvF2= M2q4T3NCVkeHUh?=
CHL-1 M2rKdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:2TWM2OD1|Lk[1O|k6KM7:TR?= MlPDV2FPT0WU
LK-2 NVLDU|Y6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDnTWM2OD1|Lk[3NVM{KM7:TR?= M{nxb3NCVkeHUh?=
Hs-578-T NYPzUphsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XkTWlEPTB;Mz62O|g4OyEQvF2= MmfQV2FPT0WU
CTB-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TjcWlEPTB;Mz64NFA2OSEQvF2= MnezV2FPT0WU
ES5 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPmSHRKSzVyPUOuPFM3OzdizszN NIfFZ5ZUSU6JRWK=
A204 M3LJeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3f4TWlEPTB;Mz65NlA4PSEQvF2= MVHTRW5ITVJ?
SW780 NIWwOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknVTWM2OD1|LkmyNlQ2KM7:TR?= M2fZUnNCVkeHUh?=
EW-3 NICxSHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvEb4FPUUN3ME2zMlk5QTJ|IN88US=> MnLnV2FPT0WU
A704 NYntOI1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zZb2lEPTB;ND6yPFczOyEQvF2= Mn7KV2FPT0WU
LU-139 NEfLSVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17vRWlEPTB;ND6zNVU{PCEQvF2= MmC0V2FPT0WU
CAL-72 NGrUPGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLnTI05UUN3ME20MlQyPzR4IN88US=> NV;odnRHW0GQR1XS
D-336MG M1P2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFu1ZVhKSzVyPUSuOFY5OTdizszN NGXMU5BUSU6JRWK=
LAMA-84 NIjnfW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTBTWM2OD12LkWzN|Eh|ryP M3Kxb3NCVkeHUh?=
GI-ME-N NHzVcolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTRwNUS4NUDPxE1? MUfTRW5ITVJ?
KM-H2 NYPLO|VxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTRwNUWyNlIh|ryP NVnDTItxW0GQR1XS
NCI-H209 Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7CRlNYUUN3ME20MlU5Ojh|IN88US=> NVH6dGlOW0GQR1XS
IGROV-1 NVu3[G5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzmfIJKSzVyPUSuPFcyPjhizszN NIDaWW1USU6JRWK=
L-363 MmGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2r3b2lEPTB;ND65OlY3PSEQvF2= MVXTRW5ITVJ?
SK-MEL-3 MljaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mly0TWM2OD13LkK0NFYh|ryP NYL4O25WW0GQR1XS
HuO9 NV7YNXJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjnVIpKSzVyPUWuN|g5PDNizszN MnHOV2FPT0WU
NOS-1 MnXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7xTWM2OD13LkeyPVI4KM7:TR?= NWXaRYd7W0GQR1XS
NCI-H1770 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\iWGpMUUN3ME21Mlk2ODN{IN88US=> NETNNZVUSU6JRWK=
SF126 MmTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO0OXNKSzVyPU[uNlE1ODZizszN MV3TRW5ITVJ?
ML-2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXsXFJ{UUN3ME22MlI1QTd5IN88US=> M4HJZ3NCVkeHUh?=
CHP-134 Mn\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTPeZhIUUN3ME22MlI2OTh{IN88US=> MkL1V2FPT0WU
NCI-H1355 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HYVmlEPTB;Nj60NVc{OyEQvF2= NV;HUmNYW0GQR1XS
TE-12 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nIPWlEPTB;Nj63NlY4OSEQvF2= MYLTRW5ITVJ?
A4-Fuk M2fxb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzqZWFKSzVyPU[uO|MyPDJizszN M2PPcXNCVkeHUh?=
MV-4-11 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjWfW5KSzVyPU[uO|Y3OjZizszN M1HWPHNCVkeHUh?=
SK-UT-1 NIHmSohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjxTWM2OD14LkmxO|g1KM7:TR?= NFP6fodUSU6JRWK=
J-RT3-T3-5 MmnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7zZYk5UUN3ME23MlA4PzZ2IN88US=> MVrTRW5ITVJ?
ME-180 M2DIZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1P2fWlEPTB;Nz6xNFQxPCEQvF2= MX;TRW5ITVJ?
SK-MEL-28 NXy4VI1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLHTWM2OD15LkO3PFE6KM7:TR?= NWfvRoRjW0GQR1XS
HAL-01 M3Pnc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;uVWlEPTB;Nz60PFM1OSEQvF2= M{TK[3NCVkeHUh?=
ES8 NV;TOIpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\Ne2lEPTB;Nz62PVYzPiEQvF2= MnLGV2FPT0WU
DB NV\DUIRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjQTWM2OD16LkGxOVA1KM7:TR?= M4[0W3NCVkeHUh?=
SK-NEP-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES3UG1KSzVyPUiuOFgyPDlizszN NH\BRWRUSU6JRWK=
COR-L88 NFnOZlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2juO2lEPTB;OD61NFk5OSEQvF2= NVmyS4FHW0GQR1XS
LB1047-RCC M2H2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TkcWlEPTB;OD61NlIyOiEQvF2= MmXhV2FPT0WU
NCI-H520 NV;4Z4dVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jhPWlEPTB;OD62NlE2PyEQvF2= NYOwR2syW0GQR1XS
SW954 M1HDU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXBRXNHUUN3ME24MlY6Pzh4IN88US=> M{DZbHNCVkeHUh?=
TE-6 NEfQNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHYOHVkUUN3ME24Mlc2OTR|IN88US=> MkLVV2FPT0WU
D-283MED NVHvVZZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13YOmlEPTB;OT6wOlU{PCEQvF2= NUDyTFM{W0GQR1XS
DBTRG-05MG NYP3epNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlO3TWM2OD17LkC5OlA4KM7:TR?= M2jFUXNCVkeHUh?=
NCI-H446 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXXUIR3UUN3ME25MlI6PTJ4IN88US=> NGPHN3VUSU6JRWK=
HOS MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\sO2lEPTB;OT6zOVE{PCEQvF2= NU[xeHFkW0GQR1XS
ES4 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\MTWM2OD17LkWwOVk2KM7:TR?= M3fX[nNCVkeHUh?=
EW-13 NHPBZ2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnnTWM2OD17Lki5NFU2KM7:TR?= NUjIOldUW0GQR1XS
IST-MES1 NVnFdFg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\uPJlKSzVyPUmuPVQ2OzRizszN MWDTRW5ITVJ?
CAS-1 MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HSW2lEPTB;OT65O|Y2QSEQvF2= NVXBRXJrW0GQR1XS
EM-2 M{PwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fG[GlEPTB;MUCuNVM6OyEQvF2= MXnTRW5ITVJ?
SW948 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFyLkG4PFIh|ryP MVnTRW5ITVJ?
OAW-42 NV62NXd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LH[GlEPTB;MUCuOVI3PyEQvF2= MULTRW5ITVJ?
BE-13 NFLiVFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTWN5RjUUN3ME2xNE43PTd4IN88US=> M4\IZ3NCVkeHUh?=
KU812 MnjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTFyLkezPVEh|ryP M{nGeXNCVkeHUh?=
SK-MEL-30 NFfXcWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrLTWM2OD1zMD64PVAyKM7:TR?= NWLYUGR1W0GQR1XS
A2780 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\NW3dKSzVyPUGxMlA{ODhizszN MXfTRW5ITVJ?
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RPMI-2650 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULtXJJLUUN3ME20N{44QDF4IN88US=> NFi1OppUSU6JRWK=
SAS M3\RRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTR|Lkm1N|Qh|ryP M2LwcXNCVkeHUh?=
MDA-MB-231 MkfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DmN2lEPTB;NEOuPVYxQSEQvF2= NXvvelM2W0GQR1XS
JVM-3 M4T3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XOe2lEPTB;NESuNFU{OyEQvF2= NYPYXpFyW0GQR1XS
COLO-320-HSR MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHLNGhYUUN3ME20OE42PjN|IN88US=> M{TsT3NCVkeHUh?=
SNB75 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL5T5V[UUN3ME20OE43OTB3IN88US=> NH:4TotUSU6JRWK=
NCI-H441 NUHwWGp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\UW5R5UUN3ME20OE46OzJ6IN88US=> M2PjfXNCVkeHUh?=
HCT-116 NETw[FdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrib3dpUUN3ME20OE46QDZ6IN88US=> MWDTRW5ITVJ?
NCI-H226 NFjnR5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPLTWM2OD12NT62N|Y5KM7:TR?= NYOyZWptW0GQR1XS
CAL-33 NXP1WJlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnqOm9KSzVyPUS1MlkzOTdizszN MmDrV2FPT0WU
NCI-H1437 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTDTWM2OD12Nj6zNlEh|ryP MYTTRW5ITVJ?
HCC1187 M2PweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDSTWM2OD12Nj60NlU2KM7:TR?= Mn;SV2FPT0WU
NUGC-3 M{OxOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPqTIJKSzVyPUS2MlU4ODlizszN NEDmN|RUSU6JRWK=
T98G M4jMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr6b4VvUUN3ME20O{42PDdizszN NEW4[pdUSU6JRWK=
OVCAR-8 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rl[mlEPTB;NEeuOlg{KM7:TR?= NEOyN2FUSU6JRWK=
LB2241-RCC NH6yN29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDVSldKSzVyPUS3MlczPyEQvF2= MUPTRW5ITVJ?
NCI-H358 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\pfmlEPTB;NEiuNVE2OiEQvF2= M2XVbHNCVkeHUh?=
PANC-08-13 M1\TOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR6LkG4OVMh|ryP NFLlc3NUSU6JRWK=
KP-N-YN NUixN5dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTR6LkKxNFIh|ryP Mk\LV2FPT0WU
NCI-H1755 NHfJWVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzXWppKSzVyPUS4MlI4OjZizszN NUf1[ZoyW0GQR1XS
NCI-N87 NXizSFl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTR6LkK5PVEh|ryP M4\VTXNCVkeHUh?=

... 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]
+ Expand

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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*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).

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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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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID