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. 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 NITmSJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO5TWM2OD1yLkCxNlI2KM7:TR?= M2HBVXNCVkeHUh?=
KG-1 M320Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMEWxNlkh|ryP MX7TRW5ITVJ?
MFM-223 NXnHflBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17vUGlEPTB;MD6yNVU4PiEQvF2= MWTTRW5ITVJ?
EoL-1-cell NY\SWWNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPCTWM2OD1yLkOyPVg1KM7:TR?= NX\0[mZxW0GQR1XS
ECC10 NEjN[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW1TWM2OD1yLkOzPFk5KM7:TR?= MmD0V2FPT0WU
H-EMC-SS M3vuSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXYTWM2OD1yLkO0O|E2KM7:TR?= NIW2c|hUSU6JRWK=
AN3-CA MoPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnQOZlKSzVyPUCuOFAyOzNizszN MkPIV2FPT0WU
HuO-3N1 MmP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX6TodmUUN3ME2wMlU1PjV|IN88US=> Mle1V2FPT0WU
RT-112 NF3SVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlL6TWM2OD1yLkW0O|AyKM7:TR?= NXHFOYhZW0GQR1XS
NEC8 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT4TlZ5UUN3ME2wMlU3Ojh7IN88US=> MYXTRW5ITVJ?
D-263MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PzR2lEPTB;MD63NVE2QSEQvF2= MlnwV2FPT0WU
SW962 M2fmWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnIN29KSzVyPUCuO|g6QDhizszN M4SwfnNCVkeHUh?=
BV-173 M2DZfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHCTWM2OD1yLki0OlI{KM7:TR?= MXLTRW5ITVJ?
MFE-280 NYr1S2NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ft[WlEPTB;MD64OVg4OiEQvF2= MWfTRW5ITVJ?
HuH-7 NIqyUJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTFwMkS0OlQh|ryP M1HuXnNCVkeHUh?=
RS4-11 M2DXd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvUTWM2OD1zLkOzPFg3KM7:TR?= NYnET21VW0GQR1XS
DMS-114 NYnnXVRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HGUWlEPTB;MT6zOlc{PyEQvF2= NX[4W|VoW0GQR1XS
MSTO-211H MnrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;sR3dCUUN3ME2xMlQ4Ozd6IN88US=> NX6wPW1NW0GQR1XS
DU-145 NYP6PJRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHMTWM2OD1zLkW4NlE4KM7:TR?= M3K0PXNCVkeHUh?=
A172 NIjze5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrOO4R7UUN3ME2xMlcxOzV3IN88US=> NEDXT5dUSU6JRWK=
SBC-1 Mmi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XrPGlEPTB;Mj6wPVQh|ryP MoTJV2FPT0WU
H9 NFPIVZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoK2TWM2OD1{LkG0N|A3KM7:TR?= NV7DbIJLW0GQR1XS
NCI-SNU-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rL[GlEPTB;Mj6xPFM6PCEQvF2= M4LQbnNCVkeHUh?=
NCI-H720 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1npXWlEPTB;Mj6yNVI5OyEQvF2= NXvseW9GW0GQR1XS
HCC2218 NVvVZ4llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJwM{e5N|kh|ryP MlTEV2FPT0WU
G-401 NI\VPWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJwNEexPFkh|ryP MXjTRW5ITVJ?
MPP-89 MonjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Pt[GlEPTB;Mj60PFM3PCEQvF2= NXn2b25JW0GQR1XS
697 M4rFcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJwNkWzN|Eh|ryP NYPUN2RxW0GQR1XS
KARPAS-45 MlH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkixTWM2OD1{LkewO|Q4KM7:TR?= MVXTRW5ITVJ?
MG-63 NY\tOZJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED2RpZKSzVyPUKuPVQzPjJizszN NUnRWoRQW0GQR1XS
NTERA-S-cl-D1 NVjaeWY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHRZXExUUN3ME2zMlA{PDd{IN88US=> MlXlV2FPT0WU
G-402 NXfocIs4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfwdIdKSzVyPUOuNVI4OjdizszN NUjmWY1zW0GQR1XS
NKM-1 NW\aXW97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfMNHhKSzVyPUOuNVM2PjRizszN MkPIV2FPT0WU
RH-18 NFHmSpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYG4dWxlUUN3ME2zMlE6PTl6IN88US=> MkntV2FPT0WU
NCI-H1092 NEfUSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DQOWlEPTB;Mz6xPVY6KM7:TR?= MUPTRW5ITVJ?
RPMI-8226 MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrlTWM2OD1|LkKzOFQ4KM7:TR?= MYHTRW5ITVJ?
GAMG MnvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTKcZhVUUN3ME2zMlQ3PTd4IN88US=> MkfVV2FPT0WU
HH MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TrN2lEPTB;Mz60O|Y4PiEQvF2= NV\DOJJPW0GQR1XS
RO82-W-1 M2DVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTNwNEm4OVUh|ryP NXnMdJp3W0GQR1XS
CCRF-CEM MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe2W|BGUUN3ME2zMlUxPDh6IN88US=> MXfTRW5ITVJ?
NBsusSR NYqyb3ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;iXFhCUUN3ME2zMlY{QTZ7IN88US=> NF3pb2pUSU6JRWK=
CHL-1 NWnEWIpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG2TWM2OD1|Lk[1O|k6KM7:TR?= NGO3ZoJUSU6JRWK=
LK-2 M4TBfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\3cWlEPTB;Mz62O|E{OyEQvF2= NYXSXVVrW0GQR1XS
Hs-578-T MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XUSWlEPTB;Mz62O|g4OyEQvF2= NIPCSJpUSU6JRWK=
CTB-1 NV;INVVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;odXlSUUN3ME2zMlgxODVzIN88US=> NGjk[YdUSU6JRWK=
ES5 NH7ZeFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNwOEO2N|ch|ryP NHjSU3hUSU6JRWK=
A204 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrWTWM2OD1|LkmyNFc2KM7:TR?= MVLTRW5ITVJ?
SW780 NHS1SFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTNwOUKyOFUh|ryP NWiwUm5OW0GQR1XS
EW-3 NF7WfVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHni[GVKSzVyPUOuPVg6OjNizszN NFHwR41USU6JRWK=
A704 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfCRod[UUN3ME20MlI5PzJ|IN88US=> MX\TRW5ITVJ?
LU-139 MkG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWH3[YNkUUN3ME20MlMyPTN2IN88US=> MlX2V2FPT0WU
CAL-72 MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzkeoRKSzVyPUSuOFE4PDZizszN MWjTRW5ITVJ?
D-336MG NGW5O4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjnPXc6UUN3ME20MlQ3QDF5IN88US=> NFHEb4RUSU6JRWK=
LAMA-84 MoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvGTWM2OD12LkWzN|Eh|ryP NEGxVFVUSU6JRWK=
GI-ME-N MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTRwNUS4NUDPxE1? NELORXdUSU6JRWK=
KM-H2 M3TNT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LQN2lEPTB;ND61OVIzOiEQvF2= MnXpV2FPT0WU
NCI-H209 M1LxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPMfIx{UUN3ME20MlU5Ojh|IN88US=> NEjYcXFUSU6JRWK=
IGROV-1 Mon6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr5O3BIUUN3ME20Mlg4OTZ6IN88US=> NIHaTFFUSU6JRWK=
L-363 NX;CW2RRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTpPGVKSzVyPUSuPVY3PjVizszN M1fuV3NCVkeHUh?=
SK-MEL-3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfs[XdKSzVyPUWuNlQxPiEQvF2= MXzTRW5ITVJ?
HuO9 MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LIcWlEPTB;NT6zPFg1OyEQvF2= Mm[5V2FPT0WU
NOS-1 NV6wTGFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTVwN{K5Nlch|ryP M2PJUXNCVkeHUh?=
NCI-H1770 MnTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;TW2lEPTB;NT65OVA{OiEQvF2= NWHJRopRW0GQR1XS
SF126 M3y2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3izU2lEPTB;Nj6yNVQxPiEQvF2= NIWz[mtUSU6JRWK=
ML-2 NGH3c|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTZwMkS5O|ch|ryP NHzVToFUSU6JRWK=
CHP-134 M4S0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL4b|BKSzVyPU[uNlUyQDJizszN MlHtV2FPT0WU
NCI-H1355 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\Y[JFOUUN3ME22MlQyPzN|IN88US=> NWDQcWxGW0GQR1XS
TE-12 NFPTe2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3Geol{UUN3ME22MlczPjdzIN88US=> M{j3bnNCVkeHUh?=
A4-Fuk NFmxZo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnDTWM2OD14LkezNVQzKM7:TR?= M3vPc3NCVkeHUh?=
MV-4-11 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTZwN{[2NlYh|ryP M1:1U3NCVkeHUh?=
SK-UT-1 NYHGOZk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPnU4Q3UUN3ME22MlkyPzh2IN88US=> NGjvUmhUSU6JRWK=
J-RT3-T3-5 Mkf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTdwMEe3OlQh|ryP M1XQcnNCVkeHUh?=
ME-180 NUCwTZl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITUZYRKSzVyPUeuNVA1ODRizszN M1OzOXNCVkeHUh?=
SK-MEL-28 M{D2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTdwM{e4NVkh|ryP NXHDXYVMW0GQR1XS
HAL-01 M3[0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnlTWM2OD15LkS4N|QyKM7:TR?= M1XnSXNCVkeHUh?=
ES8 NHPXcmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPNTWM2OD15Lk[5OlI3KM7:TR?= NUjwcZhWW0GQR1XS
DB MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlywTWM2OD16LkGxOVA1KM7:TR?= MV\TRW5ITVJ?
SK-NEP-1 NWXX[3hbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n2T2lEPTB;OD60PFE1QSEQvF2= MorCV2FPT0WU
COR-L88 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRThwNUC5PFEh|ryP NIfBTYRUSU6JRWK=
LB1047-RCC NHv5[5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRThwNUKyNVIh|ryP NXXl[nNlW0GQR1XS
NCI-H520 NIfLPZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfrOYx2UUN3ME24MlYzOTV5IN88US=> NUTqZ5NbW0GQR1XS
SW954 NXPpWXlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULJSFlzUUN3ME24MlY6Pzh4IN88US=> MV3TRW5ITVJ?
TE-6 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXIWFJKUUN3ME24Mlc2OTR|IN88US=> MYfTRW5ITVJ?
D-283MED MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvHb3lsUUN3ME25MlA3PTN2IN88US=> NH\Yb|BUSU6JRWK=
DBTRG-05MG M{[xdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTlwMEm2NFch|ryP NU\DOmI5W0GQR1XS
NCI-H446 NIDwR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXyTWM2OD17LkK5OVI3KM7:TR?= MnH3V2FPT0WU
HOS NH\lXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTlwM{WxN|Qh|ryP NV3PbY1zW0GQR1XS
ES4 NUTFXplMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\EUXJKSzVyPUmuOVA2QTVizszN NVLk[mdRW0GQR1XS
EW-13 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Xp[WlEPTB;OT64PVA2PSEQvF2= NWf0d3RXW0GQR1XS
IST-MES1 NVzKN4tUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vvdWlEPTB;OT65OFU{PCEQvF2= M3jydHNCVkeHUh?=
CAS-1 NVnzfY9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7vSWtxUUN3ME25Mlk4PjV7IN88US=> NG[5[HFUSU6JRWK=
EM-2 MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnQUohMUUN3ME2xNE4yOzl|IN88US=> M17UbXNCVkeHUh?=
SW948 NHHxRnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTFyLkG4PFIh|ryP M{HTNHNCVkeHUh?=
OAW-42 M2nQNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFyLkWyOlch|ryP NUHvW|I1W0GQR1XS
BE-13 NIDsUWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TROGlEPTB;MUCuOlU4PiEQvF2= M4XHSHNCVkeHUh?=
KU812 MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXod|hTUUN3ME2xNE44OzlzIN88US=> M{SxSHNCVkeHUh?=
SK-MEL-30 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFyLki5NFEh|ryP NWXVOVQ6W0GQR1XS
A2780 MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLLTWM2OD1zMT6wN|A5KM7:TR?= NVXRXnZmW0GQR1XS
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ZR-75-30 Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPWNWZkUUN3ME20N{4xPDl|IN88US=> MkLZV2FPT0WU
GT3TKB NU\CSYkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVi1b|U2UUN3ME20N{4zPjd7IN88US=> MnLvV2FPT0WU
RPMI-2650 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFSyUlZKSzVyPUSzMlc5OTZizszN NX;tfJZRW0GQR1XS
SAS NFG3fIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXy0XZp{UUN3ME20N{46PTN2IN88US=> NHrFUYFUSU6JRWK=
MDA-MB-231 M2POZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TzUWlEPTB;NEOuPVYxQSEQvF2= NXLQVXk{W0GQR1XS
JVM-3 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXrfJZKSzVyPUS0MlA2OzNizszN NUjkO|F1W0GQR1XS
COLO-320-HSR MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTR2LkW2N|Mh|ryP MmroV2FPT0WU
SNB75 Mom1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkG3TWM2OD12ND62NVA2KM7:TR?= MlS0V2FPT0WU
NCI-H441 NHPUVYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInLVodKSzVyPUS0Mlk{OjhizszN M1r3W3NCVkeHUh?=
HCT-116 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGGwNJRKSzVyPUS0Mlk5PjhizszN NXuyNItvW0GQR1XS
NCI-H226 NFqxb2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTR3Lk[zOlgh|ryP MkC1V2FPT0WU
CAL-33 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIriSFdKSzVyPUS1MlkzOTdizszN MYrTRW5ITVJ?
NCI-H1437 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTR4LkOyNUDPxE1? M1jPN3NCVkeHUh?=
HCC1187 MnjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTSblVKSzVyPUS2MlQzPTVizszN NFPkV2FUSU6JRWK=
NUGC-3 NFPKXWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mle1TWM2OD12Nj61O|A6KM7:TR?= NXrZPZNIW0GQR1XS
T98G M4P1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;i[ItLUUN3ME20O{42PDdizszN NFjlVYlUSU6JRWK=
OVCAR-8 NUOyZ4FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nzcWlEPTB;NEeuOlg{KM7:TR?= NWLSZohpW0GQR1XS
LB2241-RCC NYnI[W5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fFdmlEPTB;NEeuO|I4KM7:TR?= MkLkV2FPT0WU
NCI-H358 M3jKR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfKTWM2OD12OD6xNVUzKM7:TR?= NYf3bGI2W0GQR1XS
PANC-08-13 M2noT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLOUo1vUUN3ME20PE4yQDV|IN88US=> NXn2U|J7W0GQR1XS
KP-N-YN NYe0cXEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWH2dJN{UUN3ME20PE4zOTB{IN88US=> MkC1V2FPT0WU
NCI-H1755 NIHiVVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4L0NmlEPTB;NEiuNlczPiEQvF2= MnfDV2FPT0WU
NCI-N87 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrJbZI1UUN3ME20PE4zQTlzIN88US=> MXrTRW5ITVJ?

... 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 individually and in order:
5% DMSO+corn oil
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