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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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.

  • 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.

    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.

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 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2D0fWlEPTB;MD6wNVIzPSEQvF2= NHTuUWlUSU6JRWK=
KG-1 MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfN[GZKSzVyPUCuNFUyOjlizszN NWTidFczW0GQR1XS
MFM-223 M{DDTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTDTWM2OD1yLkKxOVc3KM7:TR?= M3vhTXNCVkeHUh?=
EoL-1-cell MmfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTuWlh7UUN3ME2wMlMzQTh2IN88US=> NXfhU2djW0GQR1XS
ECC10 NUHL[IlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwM{O4PVgh|ryP NEXJZplUSU6JRWK=
H-EMC-SS MnTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rhemlEPTB;MD6zOFcyPSEQvF2= Mo\GV2FPT0WU
AN3-CA NIGw[2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG1V2xKSzVyPUCuOFAyOzNizszN MXLTRW5ITVJ?
HuO-3N1 NWHxeXpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PPPWlEPTB;MD61OFY2OyEQvF2= NVfyNlNvW0GQR1XS
RT-112 NEXjdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwNUS3NFEh|ryP MofVV2FPT0WU
NEC8 NUHCXlcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnDTWM2OD1yLkW2Nlg6KM7:TR?= MnK3V2FPT0WU
D-263MG M3X1emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTHTWM2OD1yLkexNVU6KM7:TR?= M{XEcHNCVkeHUh?=
SW962 MlXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrQTWM2OD1yLke4PVg5KM7:TR?= NHKyR3FUSU6JRWK=
BV-173 MkHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:xeWZ{UUN3ME2wMlg1PjJ|IN88US=> MVHTRW5ITVJ?
MFE-280 NXPvOHNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTBwOEW4O|Ih|ryP NFHkU|ZUSU6JRWK=
HuH-7 MmLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzsTWM2OD1zLkK0OFY1KM7:TR?= MWDTRW5ITVJ?
RS4-11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn72TWM2OD1zLkOzPFg3KM7:TR?= NYrWNFhKW0GQR1XS
DMS-114 M1WzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[xN3dQUUN3ME2xMlM3PzN5IN88US=> M3jvfXNCVkeHUh?=
MSTO-211H NX\JRoR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XBbmlEPTB;MT60O|M4QCEQvF2= NELXSWZUSU6JRWK=
DU-145 NEjIXJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwNUiyNVch|ryP MWrTRW5ITVJ?
A172 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTFwN{CzOVUh|ryP NEnTPFJUSU6JRWK=
SBC-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PiNmlEPTB;Mj6wPVQh|ryP M1;RN3NCVkeHUh?=
H9 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTJwMUSzNFYh|ryP NWXzWlZCW0GQR1XS
NCI-SNU-1 M2XnfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJwMUizPVQh|ryP MX3TRW5ITVJ?
NCI-H720 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DEfGlEPTB;Mj6yNVI5OyEQvF2= M4\UT3NCVkeHUh?=
HCC2218 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfke2ZyUUN3ME2yMlM4QTN7IN88US=> M2r0e3NCVkeHUh?=
G-401 NEn2WGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlziTWM2OD1{LkS3NVg6KM7:TR?= MV7TRW5ITVJ?
MPP-89 MnzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDFTWM2OD1{LkS4N|Y1KM7:TR?= Mn\OV2FPT0WU
697 M1q1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fpVGlEPTB;Mj62OVM{OSEQvF2= NYnJdpJ1W0GQR1XS
KARPAS-45 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;Pd3hwUUN3ME2yMlcxPzR5IN88US=> NX7ke3NtW0GQR1XS
MG-63 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;WTWM2OD1{Lkm0NlYzKM7:TR?= MkOxV2FPT0WU
NTERA-S-cl-D1 M1nFVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnHdlY4UUN3ME2zMlA{PDd{IN88US=> NXrVT5c6W0GQR1XS
G-402 M3TEbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjqSYdKSzVyPUOuNVI4OjdizszN M3\PXXNCVkeHUh?=
NKM-1 NXv3O4VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f6SWlEPTB;Mz6xN|U3PCEQvF2= NFzKT5FUSU6JRWK=
RH-18 NIj1XG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTNwMUm1PVgh|ryP M1XRRXNCVkeHUh?=
NCI-H1092 MkTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzCV|dxUUN3ME2zMlE6PjlizszN MXHTRW5ITVJ?
RPMI-8226 NUPHcXB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vtUWlEPTB;Mz6yN|Q1PyEQvF2= NVfpRWdDW0GQR1XS
GAMG NIHrRnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nISmlEPTB;Mz60OlU4PiEQvF2= MYDTRW5ITVJ?
HH MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTNwNEe2O|Yh|ryP NV\ycI1sW0GQR1XS
RO82-W-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfNXldKSzVyPUOuOFk5PTVizszN NGm1RVJUSU6JRWK=
CCRF-CEM NUjvcnh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nFO2lEPTB;Mz61NFQ5QCEQvF2= NXPwbIxnW0GQR1XS
NBsusSR NE\pPXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfofo1KSzVyPUOuOlM6PjlizszN NVf3dWxrW0GQR1XS
CHL-1 NHLWWGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7PVJhKUUN3ME2zMlY2Pzl7IN88US=> NEHUR2dUSU6JRWK=
LK-2 NEPpdGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTXS41ZUUN3ME2zMlY4OTN|IN88US=> Mlv2V2FPT0WU
Hs-578-T M1HPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLwW4s1UUN3ME2zMlY4QDd|IN88US=> NHS4fGVUSU6JRWK=
CTB-1 M{nKSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHPN4hKSzVyPUOuPFAxPTFizszN Mn\NV2FPT0WU
ES5 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFviSIZKSzVyPUOuPFM3OzdizszN NIXQT5hUSU6JRWK=
A204 M2DIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHweXVKSzVyPUOuPVIxPzVizszN MnXuV2FPT0WU
SW780 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jCTGlEPTB;Mz65NlI1PSEQvF2= NYWyO2VkW0GQR1XS
EW-3 NIfTc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTNwOUi5NlMh|ryP MofaV2FPT0WU
A704 M{fHcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3P5TmlEPTB;ND6yPFczOyEQvF2= MX3TRW5ITVJ?
LU-139 MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWD0NZdiUUN3ME20MlMyPTN2IN88US=> MX3TRW5ITVJ?
CAL-72 M2W2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPPTWM2OD12LkSxO|Q3KM7:TR?= MV3TRW5ITVJ?
D-336MG NXPQNYFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\pOmVkUUN3ME20MlQ3QDF5IN88US=> M3fVbXNCVkeHUh?=
LAMA-84 NU\zWZpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjiNFZvUUN3ME20MlU{OzFizszN M4L4cXNCVkeHUh?=
GI-ME-N NHXEeGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnodlhGUUN3ME20MlU1QDFizszN NFXucZFUSU6JRWK=
KM-H2 NYewbIdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzmXnNKSzVyPUSuOVUzOjJizszN NWHic2ZMW0GQR1XS
NCI-H209 NFPnTWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S5dmlEPTB;ND61PFI5OyEQvF2= M4jaXHNCVkeHUh?=
IGROV-1 NGn1c2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTLfJNKSzVyPUSuPFcyPjhizszN NGnW[HZUSU6JRWK=
L-363 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe1dlNtUUN3ME20Mlk3PjZ3IN88US=> M3XORnNCVkeHUh?=
SK-MEL-3 MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTVTWM2OD13LkK0NFYh|ryP M4LwU3NCVkeHUh?=
HuO9 Ml6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFG5ZlNKSzVyPUWuN|g5PDNizszN NU\BNoZtW0GQR1XS
NOS-1 NUjqdFhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDXeY54UUN3ME21MlczQTJ5IN88US=> NUiwUFB4W0GQR1XS
NCI-H1770 MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TES2lEPTB;NT65OVA{OiEQvF2= NGfnSZhUSU6JRWK=
SF126 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFu4fXdKSzVyPU[uNlE1ODZizszN MkS4V2FPT0WU
ML-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HYRmlEPTB;Nj6yOFk4PyEQvF2= NFLoSIFUSU6JRWK=
CHP-134 M{XGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe0coU5UUN3ME22MlI2OTh{IN88US=> MWTTRW5ITVJ?
NCI-H1355 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTZwNEG3N|Mh|ryP NWjMXHdtW0GQR1XS
TE-12 NX6wT4x1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTZwN{K2O|Eh|ryP M1;DNXNCVkeHUh?=
A4-Fuk NGLISWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjzdoZKSzVyPU[uO|MyPDJizszN MnWxV2FPT0WU
MV-4-11 M3\adWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTZwN{[2NlYh|ryP NIGzWHBUSU6JRWK=
SK-UT-1 MlPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v3dmlEPTB;Nj65NVc5PCEQvF2= Mki3V2FPT0WU
J-RT3-T3-5 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDOTWM2OD15LkC3O|Y1KM7:TR?= MkPNV2FPT0WU
ME-180 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ToPWlEPTB;Nz6xNFQxPCEQvF2= MU\TRW5ITVJ?
SK-MEL-28 M3PlfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHmTWM2OD15LkO3PFE6KM7:TR?= M4f0PXNCVkeHUh?=
HAL-01 NVzJ[nduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTdwNEizOFEh|ryP Ml3jV2FPT0WU
ES8 MkT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;4cFdVUUN3ME23MlY6PjJ4IN88US=> MkHOV2FPT0WU
DB NXrjVYU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnkU4w3UUN3ME24MlEyPTB2IN88US=> NFPqVXRUSU6JRWK=
SK-NEP-1 MlL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7CWoFKSzVyPUiuOFgyPDlizszN NYLyTXl{W0GQR1XS
COR-L88 M324NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH0PJdKSzVyPUiuOVA6QDFizszN MoXBV2FPT0WU
LB1047-RCC NVHwZ3V3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLjcFlGUUN3ME24MlUzOjF{IN88US=> MoLFV2FPT0WU
NCI-H520 Mk\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUGwVlFHUUN3ME24MlYzOTV5IN88US=> NF;QPGhUSU6JRWK=
SW954 MlXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUK4b5pqUUN3ME24MlY6Pzh4IN88US=> NUDDUGs6W0GQR1XS
TE-6 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnBVJM1UUN3ME24Mlc2OTR|IN88US=> M4faNHNCVkeHUh?=
D-283MED NEfBUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\ITWM2OD17LkC2OVM1KM7:TR?= MmLsV2FPT0WU
DBTRG-05MG MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPLTWM2OD17LkC5OlA4KM7:TR?= NX\TOI5{W0GQR1XS
NCI-H446 MkWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TpeWlEPTB;OT6yPVUzPiEQvF2= M1q4Z3NCVkeHUh?=
HOS MlvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTlwM{WxN|Qh|ryP NE[3RlZUSU6JRWK=
ES4 NETkPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTlwNUC1PVUh|ryP NITs[ndUSU6JRWK=
EW-13 M2TjeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1foe2lEPTB;OT64PVA2PSEQvF2= M2j4UnNCVkeHUh?=
IST-MES1 MnLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLuTWM2OD17Lkm0OVM1KM7:TR?= MWTTRW5ITVJ?
CAS-1 M2LhVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1W5R2lEPTB;OT65O|Y2QSEQvF2= MoSyV2FPT0WU
EM-2 M1nWWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFyLkGzPVMh|ryP MVTTRW5ITVJ?
SW948 M{jqbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTFyLkG4PFIh|ryP NH;heoVUSU6JRWK=
OAW-42 M3m4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvxTnNKSzVyPUGwMlUzPjdizszN MYrTRW5ITVJ?
BE-13 NYi4ZYlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrMTWM2OD1zMD62OVc3KM7:TR?= NVGxWnJqW0GQR1XS
KU812 MkLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHLTJlKSzVyPUGwMlc{QTFizszN NXjRN3ZPW0GQR1XS
SK-MEL-30 NHTOdHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFyLki5NFEh|ryP M4rUXHNCVkeHUh?=
A2780 NHPlWHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHGTWM2OD1zMT6wN|A5KM7:TR?= M3\wUnNCVkeHUh?=
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NCI-H2228 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HKcWlEPTB;M{GuN|I6PiEQvF2= M4XGXXNCVkeHUh?=
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KY821 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jaXWlEPTB;M{KuOlg5PCEQvF2= MX\TRW5ITVJ?
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KYSE-520 M1OzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnLepZ[UUN3ME2zOE44OThzIN88US=> NWfrOnhRW0GQR1XS
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OVCAR-3 M3P5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYqxZoJDUUN3ME2zOk4zODR3IN88US=> NHrlOlRUSU6JRWK=
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HL-60 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTRyLkm3PFMh|ryP M13DTXNCVkeHUh?=
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NCI-H2030 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHkTWM2OD12Mj60N|Y5KM7:TR?= M1L5OnNCVkeHUh?=
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ZR-75-30 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzLOpZzUUN3ME20N{4xPDl|IN88US=> M1[xTnNCVkeHUh?=
GT3TKB M3\aPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnuVnpKSzVyPUSzMlI3PzlizszN NWTjOmRxW0GQR1XS
RPMI-2650 MkK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TkS2lEPTB;NEOuO|gyPiEQvF2= NEPDTFlUSU6JRWK=
SAS Ml7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYS4[IhpUUN3ME20N{46PTN2IN88US=> NH\lVHNUSU6JRWK=
MDA-MB-231 NXi1S4hDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLGR2FiUUN3ME20N{46PjB7IN88US=> NYHoRZRVW0GQR1XS
JVM-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTR2LkC1N|Mh|ryP NXT2Z45OW0GQR1XS
COLO-320-HSR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe5cm9bUUN3ME20OE42PjN|IN88US=> M1\uNnNCVkeHUh?=
SNB75 M2O3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTR2Lk[xNFUh|ryP M3fZWHNCVkeHUh?=
NCI-H441 MkHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTR2LkmzNlgh|ryP Mne3V2FPT0WU
HCT-116 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHlOZhKSzVyPUS0Mlk5PjhizszN MVHTRW5ITVJ?
NCI-H226 NV:0bFVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXhbY1SUUN3ME20OU43OzZ6IN88US=> MlrzV2FPT0WU
CAL-33 NXXFbWZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTR3LkmyNVch|ryP MnyzV2FPT0WU
NCI-H1437 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\IbpBCUUN3ME20Ok4{OjFizszN M1;EPHNCVkeHUh?=
HCC1187 NF3nVZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTR4LkSyOVUh|ryP NYLhN2w4W0GQR1XS
NUGC-3 M1nGfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjjO4F5UUN3ME20Ok42PzB7IN88US=> MofwV2FPT0WU
T98G NGTmUotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTR5LkW0O{DPxE1? Ml71V2FPT0WU
OVCAR-8 NYL4OVdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PxcWlEPTB;NEeuOlg{KM7:TR?= MkHkV2FPT0WU
LB2241-RCC M3HOT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULSdVJ3UUN3ME20O{44OjdizszN MnXWV2FPT0WU
NCI-H358 MlLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1qwO2lEPTB;NEiuNVE2OiEQvF2= NVHwOnVuW0GQR1XS
PANC-08-13 Ml3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTR6LkG4OVMh|ryP Mmi4V2FPT0WU
KP-N-YN MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTR6LkKxNFIh|ryP NHT2U5FUSU6JRWK=
NCI-H1755 NVzZbXpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TXRmlEPTB;NEiuNlczPiEQvF2= MmDzV2FPT0WU
NCI-N87 M{fuVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\vTWM2OD12OD6yPVkyKM7:TR?= M13rRXNCVkeHUh?=

... 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:
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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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