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
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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 M{nLZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:5TWM2OD1yLkCxNlI2KM7:TR?= MnT1V2FPT0WU
KG-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwMEWxNlkh|ryP NE\zWYhUSU6JRWK=
MFM-223 MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfXOmN[UUN3ME2wMlIyPTd4IN88US=> MnHxV2FPT0WU
EoL-1-cell M1;UcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwM{K5PFQh|ryP MoOxV2FPT0WU
ECC10 MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwM{O4PVgh|ryP NVzPUJVTW0GQR1XS
H-EMC-SS NVnxTI1HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjHTWM2OD1yLkO0O|E2KM7:TR?= NIe3d3dUSU6JRWK=
AN3-CA MmH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvOUYxKSzVyPUCuOFAyOzNizszN NY\Z[21JW0GQR1XS
HuO-3N1 NITpWWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fBRmlEPTB;MD61OFY2OyEQvF2= NXjP[GF3W0GQR1XS
RT-112 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fReWlEPTB;MD61OFcxOSEQvF2= M4XvO3NCVkeHUh?=
NEC8 M3;Mfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXjSGJnUUN3ME2wMlU3Ojh7IN88US=> NFnLS4RUSU6JRWK=
D-263MG NXLqVIRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHFfWRKSzVyPUCuO|EyPTlizszN NFHjNZdUSU6JRWK=
SW962 MlS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXpZmJKSzVyPUCuO|g6QDhizszN M4DlRXNCVkeHUh?=
BV-173 NU\ocm1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwOES2NlMh|ryP NFvKbZBUSU6JRWK=
MFE-280 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwOEW4O|Ih|ryP M2jSZ3NCVkeHUh?=
HuH-7 NV2zb5R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwMkS0OlQh|ryP NGL1[5JUSU6JRWK=
RS4-11 NEPFU|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XhOWlEPTB;MT6zN|g5PiEQvF2= NYricYgzW0GQR1XS
DMS-114 NULuTplkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrKTWM2OD1zLkO2O|M4KM7:TR?= NVG1RpVRW0GQR1XS
MSTO-211H NYL4SYxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnMclNKSzVyPUGuOFc{PzhizszN NI\0UWxUSU6JRWK=
DU-145 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXETIRrUUN3ME2xMlU5OjF5IN88US=> MYPTRW5ITVJ?
A172 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;0N5NKSzVyPUGuO|A{PTVizszN MoXmV2FPT0WU
SBC-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4n6XWlEPTB;Mj6wPVQh|ryP M{W1UnNCVkeHUh?=
H9 NV;GTGZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnOcXllUUN3ME2yMlE1OzB4IN88US=> MX3TRW5ITVJ?
NCI-SNU-1 M363UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL5TWM2OD1{LkG4N|k1KM7:TR?= MWLTRW5ITVJ?
NCI-H720 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\UTG1KSzVyPUKuNlEzQDNizszN MnrMV2FPT0WU
HCC2218 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi2TWM2OD1{LkO3PVM6KM7:TR?= NWDK[VIyW0GQR1XS
G-401 NYCycoN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnNR49KSzVyPUKuOFcyQDlizszN MYrTRW5ITVJ?
MPP-89 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPPTWM2OD1{LkS4N|Y1KM7:TR?= NEDme2ZUSU6JRWK=
697 NFvXOpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVOwRYhkUUN3ME2yMlY2OzNzIN88US=> MXHTRW5ITVJ?
KARPAS-45 M1rMTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHqT5U{UUN3ME2yMlcxPzR5IN88US=> NVXJSVV[W0GQR1XS
MG-63 M{PwcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHkTWM2OD1{Lkm0NlYzKM7:TR?= NUHyTmJKW0GQR1XS
NTERA-S-cl-D1 M3;Jdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q5eWlEPTB;Mz6wN|Q4OiEQvF2= M1i3PXNCVkeHUh?=
G-402 NFixUXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXJcYN6UUN3ME2zMlEzPzJ5IN88US=> NGPiVm5USU6JRWK=
NKM-1 M4nwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTNwMUO1OlQh|ryP MkPzV2FPT0WU
RH-18 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTNwMUm1PVgh|ryP Ml[wV2FPT0WU
NCI-H1092 Mk[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTHVZVHUUN3ME2zMlE6PjlizszN NGn2W5ZUSU6JRWK=
RPMI-8226 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3mwSGlEPTB;Mz6yN|Q1PyEQvF2= NGjiVXFUSU6JRWK=
GAMG M1nidmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LK[2lEPTB;Mz60OlU4PiEQvF2= NUPpUZJZW0GQR1XS
HH NWLDV4pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED1[4RKSzVyPUOuOFc3PzZizszN NWXnTZF5W0GQR1XS
RO82-W-1 NHSzdmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[1fIhKSzVyPUOuOFk5PTVizszN NUP5cVhHW0GQR1XS
CCRF-CEM NXr1fJRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHkTWM2OD1|LkWwOFg5KM7:TR?= MXTTRW5ITVJ?
NBsusSR NVfpdmx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLERZNHUUN3ME2zMlY{QTZ7IN88US=> MXzTRW5ITVJ?
CHL-1 M{XD[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\1TWM2OD1|Lk[1O|k6KM7:TR?= MoW1V2FPT0WU
LK-2 NYWye3hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;pZmlEPTB;Mz62O|E{OyEQvF2= NInacHJUSU6JRWK=
Hs-578-T M4\5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLLNFVKSzVyPUOuOlc5PzNizszN MVvTRW5ITVJ?
CTB-1 M2TkU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFizN3lKSzVyPUOuPFAxPTFizszN NF32fHhUSU6JRWK=
ES5 Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTNwOEO2N|ch|ryP NFHiZlFUSU6JRWK=
A204 M4fN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzTfG9KSzVyPUOuPVIxPzVizszN NVywR|BiW0GQR1XS
SW780 M2X4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjwTWM2OD1|LkmyNlQ2KM7:TR?= MVPTRW5ITVJ?
EW-3 NHHycGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzodFIyUUN3ME2zMlk5QTJ|IN88US=> MVnTRW5ITVJ?
A704 MkG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTRwMki3NlMh|ryP MVzTRW5ITVJ?
LU-139 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfwTWM2OD12LkOxOVM1KM7:TR?= Mk\tV2FPT0WU
CAL-72 MoTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3wdXhKSzVyPUSuOFE4PDZizszN M13vWnNCVkeHUh?=
D-336MG MoPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorYTWM2OD12LkS2PFE4KM7:TR?= M1faWHNCVkeHUh?=
LAMA-84 NUjlSJMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[x[2lEPTB;ND61N|MyKM7:TR?= M4P5eXNCVkeHUh?=
GI-ME-N MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjPTWM2OD12LkW0PFEh|ryP M3vpPXNCVkeHUh?=
KM-H2 NGHOVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLDeJpKSzVyPUSuOVUzOjJizszN M4e0[3NCVkeHUh?=
NCI-H209 M{i5Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO0TWM2OD12LkW4Nlg{KM7:TR?= NVXa[FM1W0GQR1XS
IGROV-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3Fb4Y3UUN3ME20Mlg4OTZ6IN88US=> NF25XZVUSU6JRWK=
L-363 MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{G5fGlEPTB;ND65OlY3PSEQvF2= NXPX[4lUW0GQR1XS
SK-MEL-3 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljnTWM2OD13LkK0NFYh|ryP MmjKV2FPT0WU
HuO9 M3[yemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHOT5lqUUN3ME21MlM5QDR|IN88US=> M3nPcnNCVkeHUh?=
NOS-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTEd|lIUUN3ME21MlczQTJ5IN88US=> NVzQbodNW0GQR1XS
NCI-H1770 NIKzVGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTVwOUWwN|Ih|ryP NFT3fllUSU6JRWK=
SF126 NUnBbpdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPPZZN6UUN3ME22MlIyPDB4IN88US=> NXSwVVdsW0GQR1XS
ML-2 MmqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF76TIpKSzVyPU[uNlQ6PzdizszN MkfCV2FPT0WU
CHP-134 M12wNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrFVpV2UUN3ME22MlI2OTh{IN88US=> M{PzdHNCVkeHUh?=
NCI-H1355 M2rvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XnV2lEPTB;Nj60NVc{OyEQvF2= MUjTRW5ITVJ?
TE-12 M1\oN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjyWVNKSzVyPU[uO|I3PzFizszN MYfTRW5ITVJ?
A4-Fuk NGfneI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUS1PG1tUUN3ME22Mlc{OTR{IN88US=> NGnQZZNUSU6JRWK=
MV-4-11 NWn5VYdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\VPY1KSzVyPU[uO|Y3OjZizszN NIfCR45USU6JRWK=
SK-UT-1 M1m5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTZwOUG3PFQh|ryP M{H5RnNCVkeHUh?=
J-RT3-T3-5 NEnrUnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjVc4pKSzVyPUeuNFc4PjRizszN NVHIV5VyW0GQR1XS
ME-180 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7FTWM2OD15LkGwOFA1KM7:TR?= NV\JXmdWW0GQR1XS
SK-MEL-28 NHXxXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmriTWM2OD15LkO3PFE6KM7:TR?= NEi0OXpUSU6JRWK=
HAL-01 NFmxVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rmeGlEPTB;Nz60PFM1OSEQvF2= MWnTRW5ITVJ?
ES8 M4fid2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nRR2lEPTB;Nz62PVYzPiEQvF2= NIjGSmxUSU6JRWK=
DB NW\POIk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXETWM2OD16LkGxOVA1KM7:TR?= MoLRV2FPT0WU
SK-NEP-1 NUf2O4hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[zRY5qUUN3ME24MlQ5OTR7IN88US=> MoLQV2FPT0WU
COR-L88 Mn31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLhPGlNUUN3ME24MlUxQThzIN88US=> MnvpV2FPT0WU
LB1047-RCC M2OyW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TO[mlEPTB;OD61NlIyOiEQvF2= NFzjb|ZUSU6JRWK=
NCI-H520 NEj6OnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRThwNkKxOVch|ryP MVnTRW5ITVJ?
SW954 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWGz[JdrUUN3ME24MlY6Pzh4IN88US=> NEnrfHNUSU6JRWK=
TE-6 Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPZeIhKSzVyPUiuO|UyPDNizszN MnrDV2FPT0WU
D-283MED NWLITod2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jSS2lEPTB;OT6wOlU{PCEQvF2= MoToV2FPT0WU
DBTRG-05MG MoPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T2fWlEPTB;OT6wPVYxPyEQvF2= M17pO3NCVkeHUh?=
NCI-H446 NGfwfmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXyTWM2OD17LkK5OVI3KM7:TR?= MnjFV2FPT0WU
HOS M13SXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfrWGRKSzVyPUmuN|UyOzRizszN NH\Kd3NUSU6JRWK=
ES4 NYLk[WR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDIWY9KSzVyPUmuOVA2QTVizszN NWjDOY1yW0GQR1XS
EW-13 NICyUWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfMZ3JKSzVyPUmuPFkxPTVizszN MWDTRW5ITVJ?
IST-MES1 M4PEZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfFTWM2OD17Lkm0OVM1KM7:TR?= M1KwRXNCVkeHUh?=
CAS-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHkWWxKSzVyPUmuPVc3PTlizszN NGnSc|RUSU6JRWK=
EM-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G0ZWlEPTB;MUCuNVM6OyEQvF2= MmjaV2FPT0WU
SW948 M3q5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHhTHN4UUN3ME2xNE4yQDh{IN88US=> Ml\EV2FPT0WU
OAW-42 NX\XR2ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTpVW9KSzVyPUGwMlUzPjdizszN Mn\6V2FPT0WU
BE-13 NWPJO3Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX34NpNJUUN3ME2xNE43PTd4IN88US=> NXHzdIpSW0GQR1XS
KU812 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFyLkezPVEh|ryP NGD6UJpUSU6JRWK=
SK-MEL-30 NVHMfW1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ThN2lEPTB;MUCuPFkxOSEQvF2= NXjRcFhkW0GQR1XS
A2780 M2HYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXQc5BKSzVyPUGxMlA{ODhizszN M1fGPHNCVkeHUh?=
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ZR-75-30 NWXqeJI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj1[mhKSzVyPUSzMlA1QTNizszN MlzHV2FPT0WU
GT3TKB NIrpc2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHIZ4tKSzVyPUSzMlI3PzlizszN M4S5VnNCVkeHUh?=
RPMI-2650 NGjmVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G1c2lEPTB;NEOuO|gyPiEQvF2= MnnLV2FPT0WU
SAS MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jjR2lEPTB;NEOuPVU{PCEQvF2= MmjMV2FPT0WU
MDA-MB-231 NH7zeIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7KTWM2OD12Mz65OlA6KM7:TR?= M3fHTnNCVkeHUh?=
JVM-3 NWLUUG9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fMS2lEPTB;NESuNFU{OyEQvF2= NFTRelVUSU6JRWK=
COLO-320-HSR MlL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7NTWM2OD12ND61OlM{KM7:TR?= MnuyV2FPT0WU
SNB75 NXSydI1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LnN2lEPTB;NESuOlExPSEQvF2= MUjTRW5ITVJ?
NCI-H441 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\jTVB6UUN3ME20OE46OzJ6IN88US=> M4nuenNCVkeHUh?=
HCT-116 NY\2d2o{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7pco9NUUN3ME20OE46QDZ6IN88US=> M1nrPXNCVkeHUh?=
NCI-H226 M3zh[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T1d2lEPTB;NEWuOlM3QCEQvF2= MoCzV2FPT0WU
CAL-33 NX7MU3d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\0TWM2OD12NT65NlE4KM7:TR?= M2XDZnNCVkeHUh?=
NCI-H1437 NHLW[3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTR4LkOyNUDPxE1? NYnNXpFDW0GQR1XS
HCC1187 M3nNSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi5cYdKSzVyPUS2MlQzPTVizszN MonLV2FPT0WU
NUGC-3 M2Xjd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUG3UpVRUUN3ME20Ok42PzB7IN88US=> NX\6UYZ1W0GQR1XS
T98G MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTR5LkW0O{DPxE1? NHnTPFBUSU6JRWK=
OVCAR-8 M{GxeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W4PGlEPTB;NEeuOlg{KM7:TR?= NGnXPGpUSU6JRWK=
LB2241-RCC NWHwPI06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR5LkeyO{DPxE1? MV;TRW5ITVJ?
NCI-H358 M3zWbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn63TWM2OD12OD6xNVUzKM7:TR?= NUSydFh{W0GQR1XS
PANC-08-13 NEjJV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfVOIVKSzVyPUS4MlE5PTNizszN NGfBc5FUSU6JRWK=
KP-N-YN NWHHc4ZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDk[pVDUUN3ME20PE4zOTB{IN88US=> NGPxcpNUSU6JRWK=
NCI-H1755 NGXJcnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zK[WlEPTB;NEiuNlczPiEQvF2= Mof2V2FPT0WU
NCI-N87 NVnmPFlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDqZ4xKSzVyPUS4MlI6QTFizszN NEC4[4pUSU6JRWK=

... 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]
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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]
+ 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
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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID