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.

Size Price Stock Quantity  
In DMSO USD 98 In stock
USD 70 In stock
USD 120 In stock
USD 470 In stock

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6 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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NV3DOm1HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHoXHdMUUN3ME2wMlAyOjJ3IN88US=> NWPCSFdDW0GQR1XS
KG-1 NETQSGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDkTZRKSzVyPUCuNFUyOjlizszN MnPLV2FPT0WU
MFM-223 NViwOmVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXXXXJKSzVyPUCuNlE2PzZizszN M1;iR3NCVkeHUh?=
EoL-1-cell NWLzTowxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TtPWlEPTB;MD6zNlk5PCEQvF2= M3LydXNCVkeHUh?=
ECC10 M3q2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7wTWM2OD1yLkOzPFk5KM7:TR?= NYHCXZJJW0GQR1XS
H-EMC-SS NVrsclN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LyW2lEPTB;MD6zOFcyPSEQvF2= NFzyRnhUSU6JRWK=
AN3-CA NHPtd2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PENWlEPTB;MD60NFE{OyEQvF2= Mn7MV2FPT0WU
HuO-3N1 MmTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTXT4tKSzVyPUCuOVQ3PTNizszN NGfJXYNUSU6JRWK=
RT-112 NYGyeYVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwNUS3NFEh|ryP MoraV2FPT0WU
NEC8 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTqTWM2OD1yLkW2Nlg6KM7:TR?= NHT1ZXpUSU6JRWK=
D-263MG NWezWIEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjOTWM2OD1yLkexNVU6KM7:TR?= NHPzPZlUSU6JRWK=
SW962 M2\Ndmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXLcoZKSzVyPUCuO|g6QDhizszN M1\OZXNCVkeHUh?=
BV-173 M1n2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwOES2NlMh|ryP NHf3SFNUSU6JRWK=
MFE-280 NIrKeHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwOEW4O|Ih|ryP NGf2TWZUSU6JRWK=
HuH-7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[xTWM2OD1zLkK0OFY1KM7:TR?= MWjTRW5ITVJ?
RS4-11 NFTab5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL2VlQ3UUN3ME2xMlM{QDh4IN88US=> M3jSb3NCVkeHUh?=
DMS-114 NVXPUmlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLFWXpKSzVyPUGuN|Y4OzdizszN M4jSRXNCVkeHUh?=
MSTO-211H MmTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTp[2s5UUN3ME2xMlQ4Ozd6IN88US=> MXjTRW5ITVJ?
DU-145 Mnz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojrTWM2OD1zLkW4NlE4KM7:TR?= Ml7jV2FPT0WU
A172 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFwN{CzOVUh|ryP NVPVeYNCW0GQR1XS
SBC-1 NUfuZlF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP2cIJKSzVyPUKuNFk1KM7:TR?= M{mzTXNCVkeHUh?=
H9 M4S1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvyd2l{UUN3ME2yMlE1OzB4IN88US=> NYL4ZVBYW0GQR1XS
NCI-SNU-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJwMUizPVQh|ryP MUDTRW5ITVJ?
NCI-H720 M4C4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJwMkGyPFMh|ryP NF6wZ4xUSU6JRWK=
HCC2218 M3zBN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETPXWNKSzVyPUKuN|c6OzlizszN M1;vNHNCVkeHUh?=
G-401 NFGyfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrWVVh[UUN3ME2yMlQ4OTh7IN88US=> MWPTRW5ITVJ?
MPP-89 NEnSRWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\jTWM2OD1{LkS4N|Y1KM7:TR?= MVXTRW5ITVJ?
697 MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33Vb2lEPTB;Mj62OVM{OSEQvF2= MXrTRW5ITVJ?
KARPAS-45 NUT1UWJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwN{C3OFch|ryP M322PXNCVkeHUh?=
MG-63 NWf2TFYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DnN2lEPTB;Mj65OFI3OiEQvF2= MojGV2FPT0WU
NTERA-S-cl-D1 Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i4XmlEPTB;Mz6wN|Q4OiEQvF2= MXvTRW5ITVJ?
G-402 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHjOXhkUUN3ME2zMlEzPzJ5IN88US=> MnfwV2FPT0WU
NKM-1 NXnJUXpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\wWWpnUUN3ME2zMlE{PTZ2IN88US=> MYPTRW5ITVJ?
RH-18 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTNwMUm1PVgh|ryP M3nLVXNCVkeHUh?=
NCI-H1092 NXjiZYl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzCTWM2OD1|LkG5Olkh|ryP NIG0NnVUSU6JRWK=
RPMI-8226 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XsXWlEPTB;Mz6yN|Q1PyEQvF2= M124VnNCVkeHUh?=
GAMG NV70R4J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTNwNE[1O|Yh|ryP M1TITnNCVkeHUh?=
HH NVvycINbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnv1TWM2OD1|LkS3Olc3KM7:TR?= MnL1V2FPT0WU
RO82-W-1 NEHaPWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIKwSXFKSzVyPUOuOFk5PTVizszN MY\TRW5ITVJ?
CCRF-CEM M1vjUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{KxVGlEPTB;Mz61NFQ5QCEQvF2= MY\TRW5ITVJ?
NBsusSR MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;kT5VKSzVyPUOuOlM6PjlizszN NHS3W4hUSU6JRWK=
CHL-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPmSHNKSzVyPUOuOlU4QTlizszN NF;ucZZUSU6JRWK=
LK-2 NX;rVnhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXixVpB5UUN3ME2zMlY4OTN|IN88US=> MnvMV2FPT0WU
Hs-578-T MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLNTWM2OD1|Lk[3PFc{KM7:TR?= NYrJWXc2W0GQR1XS
CTB-1 NVLNVYFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPRW|JiUUN3ME2zMlgxODVzIN88US=> NYPBbZZCW0GQR1XS
ES5 M3XFbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnzZ5pSUUN3ME2zMlg{PjN5IN88US=> NHfWe3JUSU6JRWK=
A204 M{nZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3ZbpJKSzVyPUOuPVIxPzVizszN NH;FW3hUSU6JRWK=
SW780 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnMTWM2OD1|LkmyNlQ2KM7:TR?= NIPUPHlUSU6JRWK=
EW-3 NUj6cpJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DwWmlEPTB;Mz65PFkzOyEQvF2= NFXrdm9USU6JRWK=
A704 MlrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPrRpF6UUN3ME20MlI5PzJ|IN88US=> NX3iZXN4W0GQR1XS
LU-139 M2XIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIGzdFBKSzVyPUSuN|E2OzRizszN MmXvV2FPT0WU
CAL-72 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWX2VmliUUN3ME20MlQyPzR4IN88US=> MWfTRW5ITVJ?
D-336MG M2XIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XNPWlEPTB;ND60OlgyPyEQvF2= M{fnTXNCVkeHUh?=
LAMA-84 M{fOOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPHTWM2OD12LkWzN|Eh|ryP NEnKblNUSU6JRWK=
GI-ME-N MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHZO25KSzVyPUSuOVQ5OSEQvF2= NGrHUI1USU6JRWK=
KM-H2 M3rMbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTRwNUWyNlIh|ryP MmrpV2FPT0WU
NCI-H209 NGrCdYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTYTWM2OD12LkW4Nlg{KM7:TR?= NFHXdHJUSU6JRWK=
IGROV-1 NF;ieJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3j[XdKSzVyPUSuPFcyPjhizszN MVfTRW5ITVJ?
L-363 MmX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfGTWM2OD12Lkm2OlY2KM7:TR?= NFfVdlJUSU6JRWK=
SK-MEL-3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTVwMkSwOkDPxE1? MortV2FPT0WU
HuO9 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXT2UYNPUUN3ME21MlM5QDR|IN88US=> M{m1VHNCVkeHUh?=
NOS-1 MlTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVf6ToFjUUN3ME21MlczQTJ5IN88US=> MX3TRW5ITVJ?
NCI-H1770 NHHVdpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K0NGlEPTB;NT65OVA{OiEQvF2= MVrTRW5ITVJ?
SF126 NFPWdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXniUmVyUUN3ME22MlIyPDB4IN88US=> NV3GeVdXW0GQR1XS
ML-2 NWf4blF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHi4c|lKSzVyPU[uNlQ6PzdizszN MULTRW5ITVJ?
CHP-134 NFj2cmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTZwMkWxPFIh|ryP NFj1SoZUSU6JRWK=
NCI-H1355 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTZwNEG3N|Mh|ryP Mo\GV2FPT0WU
TE-12 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonuTWM2OD14LkeyOlcyKM7:TR?= MWPTRW5ITVJ?
A4-Fuk MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTZwN{OxOFIh|ryP NUi2SW1pW0GQR1XS
MV-4-11 M1Txemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjKXoxpUUN3ME22Mlc3PjJ4IN88US=> NWfiUI9wW0GQR1XS
SK-UT-1 Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLRTWM2OD14LkmxO|g1KM7:TR?= NUe0UolvW0GQR1XS
J-RT3-T3-5 NI[2fmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLCTWM2OD15LkC3O|Y1KM7:TR?= MWjTRW5ITVJ?
ME-180 NEDVTYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTdwMUC0NFQh|ryP MV\TRW5ITVJ?
SK-MEL-28 NX3IZ|l[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Gw[GlEPTB;Nz6zO|gyQSEQvF2= M4\qfnNCVkeHUh?=
HAL-01 MlXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTdwNEizOFEh|ryP NUL5OmRTW0GQR1XS
ES8 MkTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;sO3E6UUN3ME23MlY6PjJ4IN88US=> NXfFT4ZrW0GQR1XS
DB NUD1So9rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRThwMUG1NFQh|ryP MVXTRW5ITVJ?
SK-NEP-1 NUjUWJdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH3dGs2UUN3ME24MlQ5OTR7IN88US=> NXvpOZgyW0GQR1XS
COR-L88 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRThwNUC5PFEh|ryP MVHTRW5ITVJ?
LB1047-RCC M2O1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjsNZd6UUN3ME24MlUzOjF{IN88US=> MnnDV2FPT0WU
NCI-H520 M2q2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXToSnJFUUN3ME24MlYzOTV5IN88US=> M3;HPXNCVkeHUh?=
SW954 NF3lTXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j6TWlEPTB;OD62PVc5PiEQvF2= NHHTXG5USU6JRWK=
TE-6 NULEdFhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF62O4JKSzVyPUiuO|UyPDNizszN NUj1Vnl6W0GQR1XS
D-283MED NGHXcXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTlwME[1N|Qh|ryP MWrTRW5ITVJ?
DBTRG-05MG M1Htemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjZW4pJUUN3ME25MlA6PjB5IN88US=> MmruV2FPT0WU
NCI-H446 M3zTbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nhfmlEPTB;OT6yPVUzPiEQvF2= M364OnNCVkeHUh?=
HOS MoT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nDTGlEPTB;OT6zOVE{PCEQvF2= NYLJ[XBJW0GQR1XS
ES4 MkTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqxOFlKSzVyPUmuOVA2QTVizszN MkflV2FPT0WU
EW-13 NYjxUlVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\iTWM2OD17Lki5NFU2KM7:TR?= NGXMW5lUSU6JRWK=
IST-MES1 M4L6[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHH2[mFKSzVyPUmuPVQ2OzRizszN NITEcGdUSU6JRWK=
CAS-1 Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[3b2lEPTB;OT65O|Y2QSEQvF2= MnPIV2FPT0WU
EM-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTNTWM2OD1zMD6xN|k{KM7:TR?= M2i3[nNCVkeHUh?=
SW948 NXzXb3ZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;WTWM2OD1zMD6xPFgzKM7:TR?= MVvTRW5ITVJ?
OAW-42 NHvKUZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFyLkWyOlch|ryP NVHSUXhxW0GQR1XS
BE-13 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW3[HNVUUN3ME2xNE43PTd4IN88US=> MnnZV2FPT0WU
KU812 MlfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTFyLkezPVEh|ryP MV7TRW5ITVJ?
SK-MEL-30 MoC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LQS2lEPTB;MUCuPFkxOSEQvF2= NETONYxUSU6JRWK=
A2780 NEnJd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFzLkCzNFgh|ryP NHvjR45USU6JRWK=
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GT3TKB MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWS3N5VnUUN3ME20N{4zPjd7IN88US=> MV3TRW5ITVJ?
RPMI-2650 M33EZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzRTWM2OD12Mz63PFE3KM7:TR?= NXzuVlMyW0GQR1XS
SAS M4e4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fuOWlEPTB;NEOuPVU{PCEQvF2= NED4foxUSU6JRWK=
MDA-MB-231 M3jrdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DZ[2lEPTB;NEOuPVYxQSEQvF2= NXvFd|hRW0GQR1XS
JVM-3 Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorVTWM2OD12ND6wOVM{KM7:TR?= M3nwPHNCVkeHUh?=
COLO-320-HSR NXvtU4FvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHFSmk6UUN3ME20OE42PjN|IN88US=> MVPTRW5ITVJ?
SNB75 NIH0TmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTR2Lk[xNFUh|ryP M{m2RXNCVkeHUh?=
NCI-H441 MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTR2LkmzNlgh|ryP M3rEdHNCVkeHUh?=
HCT-116 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn35TWM2OD12ND65PFY5KM7:TR?= MmX6V2FPT0WU
NCI-H226 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;mZZFKSzVyPUS1MlY{PjhizszN NILJW|RUSU6JRWK=
CAL-33 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\EcIlKSzVyPUS1MlkzOTdizszN NUnzWXV7W0GQR1XS
NCI-H1437 M{iwSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XHOmlEPTB;NE[uN|IyKM7:TR?= NIqxb4JUSU6JRWK=
HCC1187 NFfJeFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfxWW9KSzVyPUS2MlQzPTVizszN MXLTRW5ITVJ?
NUGC-3 MkH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTFN4VKSzVyPUS2MlU4ODlizszN NYnOd5pvW0GQR1XS
T98G MlLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXUU4I4UUN3ME20O{42PDdizszN NUfCZmV{W0GQR1XS
OVCAR-8 M3;qT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXflfo1jUUN3ME20O{43QDNizszN M3;Uc3NCVkeHUh?=
LB2241-RCC Mn7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITNU|FKSzVyPUS3MlczPyEQvF2= NWnjdYJJW0GQR1XS
NCI-H358 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXDTWM2OD12OD6xNVUzKM7:TR?= MXvTRW5ITVJ?
PANC-08-13 MkTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTieWVKSzVyPUS4MlE5PTNizszN M4L6c3NCVkeHUh?=
KP-N-YN M2rUSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW4XG5KSzVyPUS4MlIyODJizszN MnfYV2FPT0WU
NCI-H1755 NIf2RXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojDTWM2OD12OD6yO|I3KM7:TR?= MmPtV2FPT0WU
NCI-N87 NGfGbodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvSXWRsUUN3ME20PE4zQTlzIN88US=> MUnTRW5ITVJ?

... 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)

  • Mass
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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 )

  • C1
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    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
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

Instructions to calculate molar mass (molecular weight) of a chemical compound:

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