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 NVnYcodFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\QU41KSzVyPUCuNFEzOjVizszN NVL3eFZYW0GQR1XS
KG-1 M4LCW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M135SmlEPTB;MD6wOVEzQSEQvF2= NXu3Omc5W0GQR1XS
MFM-223 NGHQUlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwMkG1O|Yh|ryP MmTMV2FPT0WU
EoL-1-cell MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jBV2lEPTB;MD6zNlk5PCEQvF2= MWXTRW5ITVJ?
ECC10 M1XST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;n[GlEPTB;MD6zN|g6QCEQvF2= NVLBeJlsW0GQR1XS
H-EMC-SS MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[xZ3ZpUUN3ME2wMlM1PzF3IN88US=> MoLMV2FPT0WU
AN3-CA NGTpdVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnZXHdKSzVyPUCuOFAyOzNizszN NXLtZYE1W0GQR1XS
HuO-3N1 NGrOW4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwNUS2OVMh|ryP NEPScmhUSU6JRWK=
RT-112 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwNUS3NFEh|ryP M1v1THNCVkeHUh?=
NEC8 MlHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nDdmlEPTB;MD61OlI5QSEQvF2= MX3TRW5ITVJ?
D-263MG Mli5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwN{GxOVkh|ryP NW\oPW5nW0GQR1XS
SW962 M{HGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwN{i5PFgh|ryP M{LsSXNCVkeHUh?=
BV-173 NIHOTGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjndoFKSzVyPUCuPFQ3OjNizszN MWfTRW5ITVJ?
MFE-280 NUHPSIZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwOEW4O|Ih|ryP MVvTRW5ITVJ?
HuH-7 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHMTWM2OD1zLkK0OFY1KM7:TR?= MVvTRW5ITVJ?
RS4-11 M1vsOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwM{O4PFYh|ryP MYTTRW5ITVJ?
DMS-114 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm2b3JKSzVyPUGuN|Y4OzdizszN MVrTRW5ITVJ?
MSTO-211H MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrwTWM2OD1zLkS3N|c5KM7:TR?= MUHTRW5ITVJ?
DU-145 NY\DdJlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTFwNUiyNVch|ryP Ml7mV2FPT0WU
A172 MmPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\qTWM2OD1zLkewN|U2KM7:TR?= MkC1V2FPT0WU
SBC-1 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjiOYNDUUN3ME2yMlA6PCEQvF2= NVHifWNZW0GQR1XS
H9 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnL2TWM2OD1{LkG0N|A3KM7:TR?= NFnxZ2VUSU6JRWK=
NCI-SNU-1 M{LwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHNTWM2OD1{LkG4N|k1KM7:TR?= MXPTRW5ITVJ?
NCI-H720 NUfZdpliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjRTWM2OD1{LkKxNlg{KM7:TR?= M1LT[XNCVkeHUh?=
HCC2218 NIPFO3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ewe2lEPTB;Mj6zO|k{QSEQvF2= M2XZVXNCVkeHUh?=
G-401 M4i1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XFbGlEPTB;Mj60O|E5QSEQvF2= NHnQUGlUSU6JRWK=
MPP-89 NFrnRm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\xVmlEPTB;Mj60PFM3PCEQvF2= MVPTRW5ITVJ?
697 NIrHWY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17iO2lEPTB;Mj62OVM{OSEQvF2= M4LhPXNCVkeHUh?=
KARPAS-45 NX7zOWxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJwN{C3OFch|ryP NIDNUlVUSU6JRWK=
MG-63 NUPnfHJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfSbFlKSzVyPUKuPVQzPjJizszN NIfydYNUSU6JRWK=
NTERA-S-cl-D1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDiR2tKSzVyPUOuNFM1PzJizszN M3zvcnNCVkeHUh?=
G-402 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofvTWM2OD1|LkGyO|I4KM7:TR?= MleyV2FPT0WU
NKM-1 M4LzcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfDfJFKSzVyPUOuNVM2PjRizszN M4XDNHNCVkeHUh?=
RH-18 Mmf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TuUGlEPTB;Mz6xPVU6QCEQvF2= MUjTRW5ITVJ?
NCI-H1092 NXToeHhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHnTWM2OD1|LkG5Olkh|ryP NH[zOHdUSU6JRWK=
RPMI-8226 NWT4VlJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfuc21KSzVyPUOuNlM1PDdizszN NFS1WHVUSU6JRWK=
GAMG NUP0TIdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXkdHBKSzVyPUOuOFY2PzZizszN NIH2VlVUSU6JRWK=
HH MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3W5NmlEPTB;Mz60O|Y4PiEQvF2= MV7TRW5ITVJ?
RO82-W-1 NVTCVXR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PVSWlEPTB;Mz60PVg2PSEQvF2= Mk\oV2FPT0WU
CCRF-CEM MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkD4TWM2OD1|LkWwOFg5KM7:TR?= M1r3eXNCVkeHUh?=
NBsusSR MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:xdpVKSzVyPUOuOlM6PjlizszN MWXTRW5ITVJ?
CHL-1 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLmbnJKSzVyPUOuOlU4QTlizszN NF\yWW1USU6JRWK=
LK-2 NGGwUnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zuZWlEPTB;Mz62O|E{OyEQvF2= M2L4enNCVkeHUh?=
Hs-578-T M1HJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTNwNke4O|Mh|ryP MXXTRW5ITVJ?
CTB-1 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HyVmlEPTB;Mz64NFA2OSEQvF2= MWLTRW5ITVJ?
ES5 MoL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHzSWxbUUN3ME2zMlg{PjN5IN88US=> M{\rOnNCVkeHUh?=
A204 NYezZpduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTNwOUKwO|Uh|ryP MUHTRW5ITVJ?
SW780 MnHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrGfpJlUUN3ME2zMlkzOjR3IN88US=> MWLTRW5ITVJ?
EW-3 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPodYdSUUN3ME2zMlk5QTJ|IN88US=> NH7J[mxUSU6JRWK=
A704 M{m3b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nsPGlEPTB;ND6yPFczOyEQvF2= NE\QfXBUSU6JRWK=
LU-139 M1u5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRwM{G1N|Qh|ryP NXX6N|RNW0GQR1XS
CAL-72 NUm2e2RIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\OTWM2OD12LkSxO|Q3KM7:TR?= MYrTRW5ITVJ?
D-336MG M3fPV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DM[2lEPTB;ND60OlgyPyEQvF2= MUHTRW5ITVJ?
LAMA-84 M{LNUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fpOmlEPTB;ND61N|MyKM7:TR?= NHPHPJJUSU6JRWK=
GI-ME-N MoT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHXTHhKSzVyPUSuOVQ5OSEQvF2= NXXyWlI5W0GQR1XS
KM-H2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfTTWM2OD12LkW1NlIzKM7:TR?= NWW3WmJMW0GQR1XS
NCI-H209 MmDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTRwNUiyPFMh|ryP M3K1Z3NCVkeHUh?=
IGROV-1 Mof2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTRwOEexOlgh|ryP M2DoXnNCVkeHUh?=
L-363 NIr5WopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTRwOU[2OlUh|ryP MmfzV2FPT0WU
SK-MEL-3 NUHPPHNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTVwMkSwOkDPxE1? Mke5V2FPT0WU
HuO9 NHvae3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;LPGlEPTB;NT6zPFg1OyEQvF2= MXzTRW5ITVJ?
NOS-1 NVvGdIdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnKfG5KSzVyPUWuO|I6OjdizszN M4HBWXNCVkeHUh?=
NCI-H1770 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXyTWM2OD13Lkm1NFMzKM7:TR?= MXvTRW5ITVJ?
SF126 M37vfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:5Tlh1UUN3ME22MlIyPDB4IN88US=> NYrwWlRrW0GQR1XS
ML-2 MlrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTZwMkS5O|ch|ryP M3XtcnNCVkeHUh?=
CHP-134 MnnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\XeWlEPTB;Nj6yOVE5OiEQvF2= NXnvcINMW0GQR1XS
NCI-H1355 NYTCV|M6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjDOIFqUUN3ME22MlQyPzN|IN88US=> MlLWV2FPT0WU
TE-12 NXK4VmxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX70T|djUUN3ME22MlczPjdzIN88US=> M4rHWXNCVkeHUh?=
A4-Fuk NXHR[oV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rmRWlEPTB;Nj63N|E1OiEQvF2= M3XYfXNCVkeHUh?=
MV-4-11 MkfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkO3TWM2OD14Lke2OlI3KM7:TR?= NUfC[WdjW0GQR1XS
SK-UT-1 NV7TSmVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTZwOUG3PFQh|ryP MXnTRW5ITVJ?
J-RT3-T3-5 M4C1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jUPGlEPTB;Nz6wO|c3PCEQvF2= Ml3PV2FPT0WU
ME-180 NHjXUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLhcG1KSzVyPUeuNVA1ODRizszN MkPQV2FPT0WU
SK-MEL-28 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\BOFZKSzVyPUeuN|c5OTlizszN MU\TRW5ITVJ?
HAL-01 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT4TWM2OD15LkS4N|QyKM7:TR?= M1vPN3NCVkeHUh?=
ES8 NWC4Z256T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ixT2lEPTB;Nz62PVYzPiEQvF2= NXPTOFJuW0GQR1XS
DB NUXWW|BUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L5TmlEPTB;OD6xNVUxPCEQvF2= NXfnWFVSW0GQR1XS
SK-NEP-1 NFnnXVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIm4O5hKSzVyPUiuOFgyPDlizszN MnvEV2FPT0WU
COR-L88 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PtW2lEPTB;OD61NFk5OSEQvF2= MVzTRW5ITVJ?
LB1047-RCC M3;Te2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37oWmlEPTB;OD61NlIyOiEQvF2= Mni4V2FPT0WU
NCI-H520 MkLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDKTWM2OD16Lk[yNVU4KM7:TR?= NUXiPXN1W0GQR1XS
SW954 MmLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDvTWM2OD16Lk[5O|g3KM7:TR?= NYPSdohjW0GQR1XS
TE-6 MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRThwN{WxOFMh|ryP M{PWZXNCVkeHUh?=
D-283MED MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LGNWlEPTB;OT6wOlU{PCEQvF2= MVrTRW5ITVJ?
DBTRG-05MG MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TtcmlEPTB;OT6wPVYxPyEQvF2= NFLjT3RUSU6JRWK=
NCI-H446 M2XPT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jyU2lEPTB;OT6yPVUzPiEQvF2= M4P2dnNCVkeHUh?=
HOS M4jnSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfWPGtxUUN3ME25MlM2OTN2IN88US=> NECxUlZUSU6JRWK=
ES4 NYTJ[YxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HrVmlEPTB;OT61NFU6PSEQvF2= MX\TRW5ITVJ?
EW-13 MmHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfZTWM2OD17Lki5NFU2KM7:TR?= Mn64V2FPT0WU
IST-MES1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjuZpFKSzVyPUmuPVQ2OzRizszN MkDYV2FPT0WU
CAS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInZWFZKSzVyPUmuPVc3PTlizszN NWfk[XR3W0GQR1XS
EM-2 NWTGWJVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmzb|R3UUN3ME2xNE4yOzl|IN88US=> M1LsZXNCVkeHUh?=
SW948 NHzTcllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUm0U3o3UUN3ME2xNE4yQDh{IN88US=> NHrtU4tUSU6JRWK=
OAW-42 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTFyLkWyOlch|ryP NGS1WIVUSU6JRWK=
BE-13 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYmzVlIxUUN3ME2xNE43PTd4IN88US=> NXG5XHhjW0GQR1XS
KU812 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXTTWM2OD1zMD63N|kyKM7:TR?= MmnrV2FPT0WU
SK-MEL-30 NWnqdnppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zlTGlEPTB;MUCuPFkxOSEQvF2= NV\4d5Y{W0GQR1XS
A2780 NWHZdZoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;6dIFQUUN3ME2xNU4xOzB6IN88US=> MWjTRW5ITVJ?
TGBC24TKB Mor1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn3SmU5UUN3ME2xNU4xPzN5IN88US=> MYLTRW5ITVJ?
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GT3TKB MnrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL6W41KSzVyPUSzMlI3PzlizszN MX\TRW5ITVJ?
RPMI-2650 NVO5R5BkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILUXphKSzVyPUSzMlc5OTZizszN NFXQTIRUSU6JRWK=
SAS NFLDbopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ezfmlEPTB;NEOuPVU{PCEQvF2= MonVV2FPT0WU
MDA-MB-231 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR|Lkm2NFkh|ryP MYfTRW5ITVJ?
JVM-3 MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\QZWFKSzVyPUS0MlA2OzNizszN NHz2eGRUSU6JRWK=
COLO-320-HSR NEK2N4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfaR3JPUUN3ME20OE42PjN|IN88US=> M37WR3NCVkeHUh?=
SNB75 NYPjfYlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDETWM2OD12ND62NVA2KM7:TR?= NH7kS2RUSU6JRWK=
NCI-H441 M3L5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjQcVVKSzVyPUS0Mlk{OjhizszN MYnTRW5ITVJ?
HCT-116 NEjIVndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfzTWM2OD12ND65PFY5KM7:TR?= MmnVV2FPT0WU
NCI-H226 M3vEWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\hR4ZKSzVyPUS1MlY{PjhizszN M3e0[HNCVkeHUh?=
CAL-33 NVvFeZBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\QfpZXUUN3ME20OU46OjF5IN88US=> NYPLeXBXW0GQR1XS
NCI-H1437 NHLubYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoCzTWM2OD12Nj6zNlEh|ryP MXzTRW5ITVJ?
HCC1187 M1zpXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoH1TWM2OD12Nj60NlU2KM7:TR?= MkfrV2FPT0WU
NUGC-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTR4LkW3NFkh|ryP MUDTRW5ITVJ?
T98G M{TYfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrBNpZKSzVyPUS3MlU1PyEQvF2= MVzTRW5ITVJ?
OVCAR-8 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3W0SWlEPTB;NEeuOlg{KM7:TR?= NFy4O4FUSU6JRWK=
LB2241-RCC MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[ycGlEPTB;NEeuO|I4KM7:TR?= Ml3BV2FPT0WU
NCI-H358 MkOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjXTWM2OD12OD6xNVUzKM7:TR?= MYjTRW5ITVJ?
PANC-08-13 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2mwU2lEPTB;NEiuNVg2OyEQvF2= M{HtfHNCVkeHUh?=
KP-N-YN NYf5U4J[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHZdVdKSzVyPUS4MlIyODJizszN MYXTRW5ITVJ?
NCI-H1755 NFywNmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfpSmxCUUN3ME20PE4zPzJ4IN88US=> M1\lNnNCVkeHUh?=
NCI-N87 MlTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTR6LkK5PVEh|ryP MkO5V2FPT0WU

... 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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Molecular Weight Calculator

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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