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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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)
c-Src [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
Insulin Receptor [1]
(Cell-free assay)
~25 nM 100 nM-200 nM 19.8 μM >50 μM >50 μM
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 MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHtdHhUUUN3ME2wMlAyOjJ3IN88US=> NGTleY1USU6JRWK=
KG-1 NYS0bpo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwMEWxNlkh|ryP M2K4[HNCVkeHUh?=
MFM-223 M2PN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnQTIh7UUN3ME2wMlIyPTd4IN88US=> NX;XZ|dMW0GQR1XS
EoL-1-cell NH7ac29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXnTWM2OD1yLkOyPVg1KM7:TR?= M3X5e3NCVkeHUh?=
ECC10 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTBwM{O4PVgh|ryP NHPXbJdUSU6JRWK=
H-EMC-SS M3;wRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwM{S3NVUh|ryP NX3McYJ2W0GQR1XS
AN3-CA NU\kNWVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFO0enVKSzVyPUCuOFAyOzNizszN NEnPN41USU6JRWK=
HuO-3N1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\pTWM2OD1yLkW0OlU{KM7:TR?= NGnCVGxUSU6JRWK=
RT-112 NILPbmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHEUINKSzVyPUCuOVQ4ODFizszN NEnMPY1USU6JRWK=
NEC8 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jDb2lEPTB;MD61OlI5QSEQvF2= MVXTRW5ITVJ?
D-263MG M1rZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T4R2lEPTB;MD63NVE2QSEQvF2= NV;KfWlzW0GQR1XS
SW962 NFPre45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIT2O45KSzVyPUCuO|g6QDhizszN Mmr2V2FPT0WU
BV-173 NW\LXlJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzjVnZKSzVyPUCuPFQ3OjNizszN MoHzV2FPT0WU
MFE-280 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr5b2VJUUN3ME2wMlg2QDd{IN88US=> NUT1RotXW0GQR1XS
HuH-7 M3zoeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnNTWM2OD1zLkK0OFY1KM7:TR?= NXrZbWVXW0GQR1XS
RS4-11 MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwM{O4PFYh|ryP M4W0[3NCVkeHUh?=
DMS-114 Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rm[GlEPTB;MT6zOlc{PyEQvF2= MYnTRW5ITVJ?
MSTO-211H M4q4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfBTWM2OD1zLkS3N|c5KM7:TR?= M3u5T3NCVkeHUh?=
DU-145 M3n5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3hTWM2OD1zLkW4NlE4KM7:TR?= MmLSV2FPT0WU
A172 NYLIUGdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnuzTWM2OD1zLkewN|U2KM7:TR?= M3rnUXNCVkeHUh?=
SBC-1 Ml7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnlc2k2UUN3ME2yMlA6PCEQvF2= MX;TRW5ITVJ?
H9 M2fF[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTJwMUSzNFYh|ryP NXnIVmVqW0GQR1XS
NCI-SNU-1 MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOxZ2lVUUN3ME2yMlE5Ozl2IN88US=> MmP4V2FPT0WU
NCI-H720 NF3VOVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkniTWM2OD1{LkKxNlg{KM7:TR?= MXjTRW5ITVJ?
HCC2218 MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H0[GlEPTB;Mj6zO|k{QSEQvF2= M{CxdXNCVkeHUh?=
G-401 NUP0U2g1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;GTnI1UUN3ME2yMlQ4OTh7IN88US=> NYPiNWMzW0GQR1XS
MPP-89 NIjpV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPvTWM2OD1{LkS4N|Y1KM7:TR?= NX;rbnMxW0GQR1XS
697 NH2y[VdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nYcmlEPTB;Mj62OVM{OSEQvF2= MWfTRW5ITVJ?
KARPAS-45 M1XX[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnWN2dKSzVyPUKuO|A4PDdizszN M{W2W3NCVkeHUh?=
MG-63 NHPXTZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJwOUSyOlIh|ryP MV\TRW5ITVJ?
NTERA-S-cl-D1 M4rIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{naT2lEPTB;Mz6wN|Q4OiEQvF2= NFO5T5hUSU6JRWK=
G-402 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTNwMUK3Nlch|ryP Ml7PV2FPT0WU
NKM-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;zVHdKSzVyPUOuNVM2PjRizszN NHfFfWdUSU6JRWK=
RH-18 NWizeYRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTNwMUm1PVgh|ryP M2OwfnNCVkeHUh?=
NCI-H1092 Ml\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULkPWhbUUN3ME2zMlE6PjlizszN M{DFRnNCVkeHUh?=
RPMI-8226 Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nxUWlEPTB;Mz6yN|Q1PyEQvF2= Mm\BV2FPT0WU
GAMG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDXTWM2OD1|LkS2OVc3KM7:TR?= M2LDNnNCVkeHUh?=
HH NX\SeVluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfVT2VKSzVyPUOuOFc3PzZizszN MnywV2FPT0WU
RO82-W-1 NXvCd5FrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTNwNEm4OVUh|ryP MYjTRW5ITVJ?
CCRF-CEM MmDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnuyTWM2OD1|LkWwOFg5KM7:TR?= MlvnV2FPT0WU
NBsusSR MkXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XZfmlEPTB;Mz62N|k3QSEQvF2= NHiwbJRUSU6JRWK=
CHL-1 NYD0Smo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmzSVJMUUN3ME2zMlY2Pzl7IN88US=> MXrTRW5ITVJ?
LK-2 NH\ESlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTNwNkexN|Mh|ryP MoTTV2FPT0WU
Hs-578-T NICwSG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K4R2lEPTB;Mz62O|g4OyEQvF2= NFHYe5NUSU6JRWK=
CTB-1 M1fOTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7SbWI5UUN3ME2zMlgxODVzIN88US=> M2j5bHNCVkeHUh?=
ES5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\oeJlRUUN3ME2zMlg{PjN5IN88US=> NY\GOWRIW0GQR1XS
A204 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1qwZWlEPTB;Mz65NlA4PSEQvF2= NVTSPXN7W0GQR1XS
SW780 NFfsWlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\VTWM2OD1|LkmyNlQ2KM7:TR?= NH;5[3FUSU6JRWK=
EW-3 MoDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIiy[ZdKSzVyPUOuPVg6OjNizszN MXPTRW5ITVJ?
A704 MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PBdWlEPTB;ND6yPFczOyEQvF2= NEXodopUSU6JRWK=
LU-139 MlPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHMTWM2OD12LkOxOVM1KM7:TR?= M3THWHNCVkeHUh?=
CAL-72 NH3lN3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPUZnJpUUN3ME20MlQyPzR4IN88US=> MUfTRW5ITVJ?
D-336MG MlPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjQO|dKSzVyPUSuOFY5OTdizszN Mne0V2FPT0WU
LAMA-84 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;jXnZpUUN3ME20MlU{OzFizszN MmSzV2FPT0WU
GI-ME-N M1HwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLpe4hKSzVyPUSuOVQ5OSEQvF2= NIHjUIdUSU6JRWK=
KM-H2 MkG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\CZWkzUUN3ME20MlU2OjJ{IN88US=> NEn4fnZUSU6JRWK=
NCI-H209 M1vEWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTRwNUiyPFMh|ryP NHnGNoVUSU6JRWK=
IGROV-1 Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPSTJR1UUN3ME20Mlg4OTZ6IN88US=> NF\SVmtUSU6JRWK=
L-363 M1;tdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojVTWM2OD12Lkm2OlY2KM7:TR?= MmXNV2FPT0WU
SK-MEL-3 M1L4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mni4TWM2OD13LkK0NFYh|ryP M1LuNXNCVkeHUh?=
HuO9 NXrCfHdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{D3SmlEPTB;NT6zPFg1OyEQvF2= NWLGd4V3W0GQR1XS
NOS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XMe2lEPTB;NT63NlkzPyEQvF2= NVTIN|Z1W0GQR1XS
NCI-H1770 NIr1O21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTVwOUWwN|Ih|ryP M1XkSXNCVkeHUh?=
SF126 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nmWmlEPTB;Nj6yNVQxPiEQvF2= MnzqV2FPT0WU
ML-2 M4mxfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTZwMkS5O|ch|ryP Ml7iV2FPT0WU
CHP-134 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTZwMkWxPFIh|ryP MnT3V2FPT0WU
NCI-H1355 M13Ldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTZwNEG3N|Mh|ryP MmHtV2FPT0WU
TE-12 Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f3VGlEPTB;Nj63NlY4OSEQvF2= NXXze2o4W0GQR1XS
A4-Fuk Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELLV4hKSzVyPU[uO|MyPDJizszN NIjMVJFUSU6JRWK=
MV-4-11 NGn5N2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXlZ2hFUUN3ME22Mlc3PjJ4IN88US=> NX7GeIZuW0GQR1XS
SK-UT-1 MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHjUnN5UUN3ME22MlkyPzh2IN88US=> NVi3ell{W0GQR1XS
J-RT3-T3-5 M4Txc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTROHBKSzVyPUeuNFc4PjRizszN MkXRV2FPT0WU
ME-180 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr1TYlKSzVyPUeuNVA1ODRizszN NHnPU3hUSU6JRWK=
SK-MEL-28 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\1TWM2OD15LkO3PFE6KM7:TR?= MmL0V2FPT0WU
HAL-01 M3XSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHBXnJKSzVyPUeuOFg{PDFizszN NEL1d2xUSU6JRWK=
ES8 NWTOR4s6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLwTWM2OD15Lk[5OlI3KM7:TR?= MmLoV2FPT0WU
DB MojGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYKxW25pUUN3ME24MlEyPTB2IN88US=> MX\TRW5ITVJ?
SK-NEP-1 NGPW[|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXq5Z5RwUUN3ME24MlQ5OTR7IN88US=> NIjqPVlUSU6JRWK=
COR-L88 M1Hqdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjLTWM2OD16LkWwPVgyKM7:TR?= MWXTRW5ITVJ?
LB1047-RCC NIXHSW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TNeGlEPTB;OD61NlIyOiEQvF2= NWTRdpFXW0GQR1XS
NCI-H520 M2P0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH74VXpKSzVyPUiuOlIyPTdizszN MomyV2FPT0WU
SW954 NHrYSmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRThwNkm3PFYh|ryP MmDwV2FPT0WU
TE-6 M4X0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDpTWM2OD16Lke1NVQ{KM7:TR?= NYL5NIo{W0GQR1XS
D-283MED M1jWVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkD4TWM2OD17LkC2OVM1KM7:TR?= MmT5V2FPT0WU
DBTRG-05MG MoXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorjTWM2OD17LkC5OlA4KM7:TR?= MoDrV2FPT0WU
NCI-H446 M{XvT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnOTWM2OD17LkK5OVI3KM7:TR?= MWfTRW5ITVJ?
HOS MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYK5PXZlUUN3ME25MlM2OTN2IN88US=> NI\tWWFUSU6JRWK=
ES4 NUTicWpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz2TWM2OD17LkWwOVk2KM7:TR?= MUXTRW5ITVJ?
EW-13 MnHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTlwOEmwOVUh|ryP NXn0T2FUW0GQR1XS
IST-MES1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTlwOUS1N|Qh|ryP NFW5c|dUSU6JRWK=
CAS-1 NH:zUWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTlwOUe2OVkh|ryP M{Dlb3NCVkeHUh?=
EM-2 MljIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTFyLkGzPVMh|ryP NI\KfnZUSU6JRWK=
SW948 NV24d3NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XCS2lEPTB;MUCuNVg5OiEQvF2= NWjhT3ZtW0GQR1XS
OAW-42 NYT4fZY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfiTWM2OD1zMD61NlY4KM7:TR?= MWLTRW5ITVJ?
BE-13 M{fNbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\SPGlKSzVyPUGwMlY2PzZizszN M2LDV3NCVkeHUh?=
KU812 NGnJTGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HBSWlEPTB;MUCuO|M6OSEQvF2= MX7TRW5ITVJ?
SK-MEL-30 NEfUPYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\3VmFKSzVyPUGwMlg6ODFizszN NWHHOnA4W0GQR1XS
A2780 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[4O2lEPTB;MUGuNFMxQCEQvF2= NHi5[JlUSU6JRWK=
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ZR-75-30 NILnPVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTR|LkC0PVMh|ryP M1HPbXNCVkeHUh?=
GT3TKB MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PjVGlEPTB;NEOuNlY4QSEQvF2= Mme3V2FPT0WU
RPMI-2650 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDSeHFKSzVyPUSzMlc5OTZizszN NYDK[m5tW0GQR1XS
SAS MmnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K0bWlEPTB;NEOuPVU{PCEQvF2= M4D1SHNCVkeHUh?=
MDA-MB-231 M1zPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYD6[5hkUUN3ME20N{46PjB7IN88US=> NHvKZWlUSU6JRWK=
JVM-3 NH;WWFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnKcZdHUUN3ME20OE4xPTN|IN88US=> NFix[|hUSU6JRWK=
COLO-320-HSR MnXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\XTWM2OD12ND61OlM{KM7:TR?= MVvTRW5ITVJ?
SNB75 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLyNWVTUUN3ME20OE43OTB3IN88US=> MWHTRW5ITVJ?
NCI-H441 MkLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\WTWM2OD12ND65N|I5KM7:TR?= M3G0[nNCVkeHUh?=
HCT-116 NHu2XFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LzcmlEPTB;NESuPVg3QCEQvF2= M{Gz[nNCVkeHUh?=
NCI-H226 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTR3Lk[zOlgh|ryP MWnTRW5ITVJ?
CAL-33 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvhblRKSzVyPUS1MlkzOTdizszN M4jjfHNCVkeHUh?=
NCI-H1437 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX3RWJpUUN3ME20Ok4{OjFizszN NXXNSXJJW0GQR1XS
HCC1187 NGjTUHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTR4LkSyOVUh|ryP NGW0RnRUSU6JRWK=
NUGC-3 NYHQV41sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFewW4FKSzVyPUS2MlU4ODlizszN NYXyN4gxW0GQR1XS
T98G NUDhVVdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf6[3RKSzVyPUS3MlU1PyEQvF2= MYLTRW5ITVJ?
OVCAR-8 NWjOSnJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\lTWM2OD12Nz62PFMh|ryP Mnf6V2FPT0WU
LB2241-RCC M3fxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjoTYNKSzVyPUS3MlczPyEQvF2= M2LsfHNCVkeHUh?=
NCI-H358 NHXM[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTJTWM2OD12OD6xNVUzKM7:TR?= MkfuV2FPT0WU
PANC-08-13 NUHjT45CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTR6LkG4OVMh|ryP MUfTRW5ITVJ?
KP-N-YN M2fN[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLlTWM2OD12OD6yNVAzKM7:TR?= M3nm[HNCVkeHUh?=
NCI-H1755 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;rTJBKSzVyPUS4MlI4OjZizszN NV\tcHhUW0GQR1XS
NCI-N87 NX32RlUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXUUmZKSzVyPUS4MlI6QTFizszN MUTTRW5ITVJ?

... 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 <1 mg/mL
In vivo 5% DMSO+corn oil 15mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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).

Dilution Calculator

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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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID