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.

  • 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 Ml;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjXWXVKSzVyPUCuNFEzOjVizszN M4DNSHNCVkeHUh?=
KG-1 NVj3b3V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLQVFNKSzVyPUCuNFUyOjlizszN NG[1d4NUSU6JRWK=
MFM-223 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHhNmxKSzVyPUCuNlE2PzZizszN NV\MN4lwW0GQR1XS
EoL-1-cell MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nGV2lEPTB;MD6zNlk5PCEQvF2= MV\TRW5ITVJ?
ECC10 NUn2bVlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PqSWlEPTB;MD6zN|g6QCEQvF2= MnTlV2FPT0WU
H-EMC-SS NULoT4Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHnTWM2OD1yLkO0O|E2KM7:TR?= NVTJUY5sW0GQR1XS
AN3-CA M4DV[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX6TWM2OD1yLkSwNVM{KM7:TR?= M3LLWXNCVkeHUh?=
HuO-3N1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfUSlZKSzVyPUCuOVQ3PTNizszN M1XIc3NCVkeHUh?=
RT-112 NWTWNHNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fnTGlEPTB;MD61OFcxOSEQvF2= NV3hU4Z{W0GQR1XS
NEC8 NHm4RWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TpfWlEPTB;MD61OlI5QSEQvF2= NXfTU29NW0GQR1XS
D-263MG NUC5SZo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jQbmlEPTB;MD63NVE2QSEQvF2= NV7CN5hsW0GQR1XS
SW962 MnPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHkdnlKSzVyPUCuO|g6QDhizszN MY\TRW5ITVJ?
BV-173 M4qzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\4cFdKSzVyPUCuPFQ3OjNizszN NVP1dYdrW0GQR1XS
MFE-280 M{\v[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TpcGlEPTB;MD64OVg4OiEQvF2= M3[xPHNCVkeHUh?=
HuH-7 NVzmPFFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjsSlYxUUN3ME2xMlI1PDZ2IN88US=> NGjhPXdUSU6JRWK=
RS4-11 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlyyTWM2OD1zLkOzPFg3KM7:TR?= MXjTRW5ITVJ?
DMS-114 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jpN2lEPTB;MT6zOlc{PyEQvF2= NYrQboI1W0GQR1XS
MSTO-211H MnL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwNEezO|gh|ryP NYjE[2M5W0GQR1XS
DU-145 M2fqVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rST2lEPTB;MT61PFIyPyEQvF2= M3j1eXNCVkeHUh?=
A172 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTjfWJVUUN3ME2xMlcxOzV3IN88US=> NYf1bJdIW0GQR1XS
SBC-1 MoHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTJwMEm0JO69VQ>? MX;TRW5ITVJ?
H9 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTJwMUSzNFYh|ryP Mo\2V2FPT0WU
NCI-SNU-1 NHHHb3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Hje2lEPTB;Mj6xPFM6PCEQvF2= NHfSOm5USU6JRWK=
NCI-H720 NUH1TnZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL5V|hKSzVyPUKuNlEzQDNizszN NXLqU41PW0GQR1XS
HCC2218 M1r2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJwM{e5N|kh|ryP M3m4NHNCVkeHUh?=
G-401 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jrbWlEPTB;Mj60O|E5QSEQvF2= MUHTRW5ITVJ?
MPP-89 NHq4dZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJwNEizOlQh|ryP NITKSJlUSU6JRWK=
697 NHLIbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIT3d2VKSzVyPUKuOlU{OzFizszN Mme4V2FPT0WU
KARPAS-45 M4TVWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C5c2lEPTB;Mj63NFc1PyEQvF2= NXnMZoVzW0GQR1XS
MG-63 Ml7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPIeFJKSzVyPUKuPVQzPjJizszN NV3mTmJlW0GQR1XS
NTERA-S-cl-D1 NF36NZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fFPWlEPTB;Mz6wN|Q4OiEQvF2= NFe5T4NUSU6JRWK=
G-402 NIixVHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{mxS2lEPTB;Mz6xNlczPyEQvF2= NVf6OJZKW0GQR1XS
NKM-1 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTNwMUO1OlQh|ryP MV;TRW5ITVJ?
RH-18 MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDWV|JzUUN3ME2zMlE6PTl6IN88US=> Mn3xV2FPT0WU
NCI-H1092 NV\5e5h1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoT6TWM2OD1|LkG5Olkh|ryP MlfBV2FPT0WU
RPMI-8226 NXXqTHJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojQTWM2OD1|LkKzOFQ4KM7:TR?= Mlj1V2FPT0WU
GAMG NFS4OZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXCWo9EUUN3ME2zMlQ3PTd4IN88US=> M{S4SHNCVkeHUh?=
HH Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP4TWM2OD1|LkS3Olc3KM7:TR?= M2HUO3NCVkeHUh?=
RO82-W-1 MorvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPVdpVuUUN3ME2zMlQ6QDV3IN88US=> NV\aN49vW0GQR1XS
CCRF-CEM MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:yd5FKSzVyPUOuOVA1QDhizszN NEntNZBUSU6JRWK=
NBsusSR MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LRRWlEPTB;Mz62N|k3QSEQvF2= MorZV2FPT0WU
CHL-1 M4rXfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGWwVWdKSzVyPUOuOlU4QTlizszN M2nPfnNCVkeHUh?=
LK-2 NYfZZnR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n1XGlEPTB;Mz62O|E{OyEQvF2= M4HMcHNCVkeHUh?=
Hs-578-T NYrscFdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnqzTWM2OD1|Lk[3PFc{KM7:TR?= NVTvOHJsW0GQR1XS
CTB-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PoTWlEPTB;Mz64NFA2OSEQvF2= NUL3eWlHW0GQR1XS
ES5 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnT6TWM2OD1|LkizOlM4KM7:TR?= NELrOYNUSU6JRWK=
A204 NFrIUJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTNwOUKwO|Uh|ryP NYe1XGZ5W0GQR1XS
SW780 NUPwSoxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTNwOUKyOFUh|ryP MUjTRW5ITVJ?
EW-3 NHnZR3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTNwOUi5NlMh|ryP Mn65V2FPT0WU
A704 M3u5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDoW2FKSzVyPUSuNlg4OjNizszN M2rSOnNCVkeHUh?=
LU-139 NFnuW5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\i[mlKSzVyPUSuN|E2OzRizszN MYXTRW5ITVJ?
CAL-72 M16wfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\XSGx{UUN3ME20MlQyPzR4IN88US=> NWfXc2g2W0GQR1XS
D-336MG NWLkZ2w5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYO5WJNPUUN3ME20MlQ3QDF5IN88US=> M2XmZnNCVkeHUh?=
LAMA-84 M37EN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS3SWd4UUN3ME20MlU{OzFizszN M1\jNXNCVkeHUh?=
GI-ME-N MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTRwNUS4NUDPxE1? MYjTRW5ITVJ?
KM-H2 NH75b3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXGwXY1rUUN3ME20MlU2OjJ{IN88US=> NFKwfIdUSU6JRWK=
NCI-H209 M{nXeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTRwNUiyPFMh|ryP NIH0WZRUSU6JRWK=
IGROV-1 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLVTWM2OD12Lki3NVY5KM7:TR?= M1;qTHNCVkeHUh?=
L-363 NV30[4lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPu[3BKSzVyPUSuPVY3PjVizszN M3HzS3NCVkeHUh?=
SK-MEL-3 NV\zVIRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTVwMkSwOkDPxE1? NI\2OGlUSU6JRWK=
HuO9 M3;2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTVwM{i4OFMh|ryP M{PNZnNCVkeHUh?=
NOS-1 M4TkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;rOoU{UUN3ME21MlczQTJ5IN88US=> M1S3S3NCVkeHUh?=
NCI-H1770 NEW5O2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nje2lEPTB;NT65OVA{OiEQvF2= Ml;RV2FPT0WU
SF126 NV\p[nFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfuTWM2OD14LkKxOFA3KM7:TR?= M{D6SnNCVkeHUh?=
ML-2 NF7MfItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUK3VYpvUUN3ME22MlI1QTd5IN88US=> M3\UWHNCVkeHUh?=
CHP-134 MnTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfLTWM2OD14LkK1NVgzKM7:TR?= MVHTRW5ITVJ?
NCI-H1355 NE\NOXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOyTWM2OD14LkSxO|M{KM7:TR?= MnjVV2FPT0WU
TE-12 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nkVWlEPTB;Nj63NlY4OSEQvF2= M2\mXXNCVkeHUh?=
A4-Fuk NVTDdmYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPiTWM2OD14LkezNVQzKM7:TR?= MkH3V2FPT0WU
MV-4-11 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;sTWM2OD14Lke2OlI3KM7:TR?= NUj6TW8yW0GQR1XS
SK-UT-1 M3O0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHITWM2OD14LkmxO|g1KM7:TR?= M2\YbHNCVkeHUh?=
J-RT3-T3-5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rMOWlEPTB;Nz6wO|c3PCEQvF2= M1L3fHNCVkeHUh?=
ME-180 NU\RdGszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPTTWM2OD15LkGwOFA1KM7:TR?= MWLTRW5ITVJ?
SK-MEL-28 NFLBd21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzpWHJKSzVyPUeuN|c5OTlizszN MUXTRW5ITVJ?
HAL-01 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHOS3hQUUN3ME23MlQ5OzRzIN88US=> NV;XXXNlW0GQR1XS
ES8 MoDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L0fGlEPTB;Nz62PVYzPiEQvF2= NY\BZVlNW0GQR1XS
DB MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13Uc2lEPTB;OD6xNVUxPCEQvF2= M3GyenNCVkeHUh?=
SK-NEP-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTxTWM2OD16LkS4NVQ6KM7:TR?= NYPTTVliW0GQR1XS
COR-L88 M3TlVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX4UVBKSzVyPUiuOVA6QDFizszN NGOyfYRUSU6JRWK=
LB1047-RCC M{TWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\qdXdKSzVyPUiuOVIzOTJizszN MnLtV2FPT0WU
NCI-H520 NXjyfmY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\LRWlEPTB;OD62NlE2PyEQvF2= Mm\RV2FPT0WU
SW954 NF7MOFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m4V2lEPTB;OD62PVc5PiEQvF2= MkXmV2FPT0WU
TE-6 M4\neWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTOUJFKSzVyPUiuO|UyPDNizszN MXzTRW5ITVJ?
D-283MED MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTlwME[1N|Qh|ryP NY\5blJ1W0GQR1XS
DBTRG-05MG NXv0Z5p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTlwMEm2NFch|ryP MoC2V2FPT0WU
NCI-H446 M{LscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmWwTWM2OD17LkK5OVI3KM7:TR?= NGXTXFdUSU6JRWK=
HOS NUXJ[|ZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\CN2FKSzVyPUmuN|UyOzRizszN NVrufoNxW0GQR1XS
ES4 M2f5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Lxd2lEPTB;OT61NFU6PSEQvF2= M3zNdHNCVkeHUh?=
EW-13 NUi0[ZZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLt[ZpKSzVyPUmuPFkxPTVizszN MYDTRW5ITVJ?
IST-MES1 NWrnXoNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS2TWM2OD17Lkm0OVM1KM7:TR?= M4nRV3NCVkeHUh?=
CAS-1 NXK5NWNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL1O5dKSzVyPUmuPVc3PTlizszN M325OHNCVkeHUh?=
EM-2 NYfkOnpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPyT|JRUUN3ME2xNE4yOzl|IN88US=> NUHPbFhPW0GQR1XS
SW948 NUH2SHE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFyLkG4PFIh|ryP NUXPN3REW0GQR1XS
OAW-42 NGLq[G5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFyLkWyOlch|ryP NWXGUWpoW0GQR1XS
BE-13 NXewToxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;3TmlEPTB;MUCuOlU4PiEQvF2= NGHJZ|JUSU6JRWK=
KU812 NYfCT3loT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFyLkezPVEh|ryP NF;SOYlUSU6JRWK=
SK-MEL-30 NVribpV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjqVXRKSzVyPUGwMlg6ODFizszN MmfPV2FPT0WU
A2780 NHP4S|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\jSXBDUUN3ME2xNU4xOzB6IN88US=> NWP0O5gxW0GQR1XS
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GT3TKB M3vX[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH1OIlKSzVyPUSzMlI3PzlizszN MVXTRW5ITVJ?
RPMI-2650 MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTVTWM2OD12Mz63PFE3KM7:TR?= MknQV2FPT0WU
SAS MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonzTWM2OD12Mz65OVM1KM7:TR?= MVTTRW5ITVJ?
MDA-MB-231 NU\HWnFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWG3XWJYUUN3ME20N{46PjB7IN88US=> NXX1Z4drW0GQR1XS
JVM-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR2LkC1N|Mh|ryP MXvTRW5ITVJ?
COLO-320-HSR MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljSTWM2OD12ND61OlM{KM7:TR?= MV7TRW5ITVJ?
SNB75 NXHVU|dNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTR2Lk[xNFUh|ryP NVjZPFZUW0GQR1XS
NCI-H441 NHjTe4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK3b4VKSzVyPUS0Mlk{OjhizszN MVLTRW5ITVJ?
HCT-116 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR2Lkm4Olgh|ryP Ml\xV2FPT0WU
NCI-H226 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[1TWM2OD12NT62N|Y5KM7:TR?= MorpV2FPT0WU
CAL-33 MoLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHudYloUUN3ME20OU46OjF5IN88US=> NVS1bXY{W0GQR1XS
NCI-H1437 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTR4LkOyNUDPxE1? M1XMUHNCVkeHUh?=
HCC1187 NVi3[YZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HoWGlEPTB;NE[uOFI2PSEQvF2= NXzrSJN{W0GQR1XS
NUGC-3 NIn5fo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXNRY1KSzVyPUS2MlU4ODlizszN MV;TRW5ITVJ?
T98G M2HLTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR5LkW0O{DPxE1? NUjPZYIxW0GQR1XS
OVCAR-8 NEPXc4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvqTWM2OD12Nz62PFMh|ryP Mm[zV2FPT0WU
LB2241-RCC MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO5UoZuUUN3ME20O{44OjdizszN M3rsVHNCVkeHUh?=
NCI-H358 NUPieJZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLiTWM2OD12OD6xNVUzKM7:TR?= NFzyVJFUSU6JRWK=
PANC-08-13 NX\2WHRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTqU2w1UUN3ME20PE4yQDV|IN88US=> NIi5PVJUSU6JRWK=
KP-N-YN MmS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz3TWM2OD12OD6yNVAzKM7:TR?= NGXZbotUSU6JRWK=
NCI-H1755 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTR6LkK3NlYh|ryP MXXTRW5ITVJ?
NCI-N87 M3fv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnntTWM2OD12OD6yPVkyKM7:TR?= M4TyfnNCVkeHUh?=

... 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:

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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

FGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID