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 NED1R5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH0V3RKSzVyPUCuNFEzOjVizszN NFXZdHpUSU6JRWK=
KG-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMEWxNlkh|ryP MYHTRW5ITVJ?
MFM-223 NFLPWZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnwflhKSzVyPUCuNlE2PzZizszN NXPqd29wW0GQR1XS
EoL-1-cell MlnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHSRopKSzVyPUCuN|I6QDRizszN M3XHUXNCVkeHUh?=
ECC10 NHmxOJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTzelc{UUN3ME2wMlM{QDl6IN88US=> MlzBV2FPT0WU
H-EMC-SS M{LP[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTzPFZKSzVyPUCuN|Q4OTVizszN NFLQ[WJUSU6JRWK=
AN3-CA M4SwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwNECxN|Mh|ryP M4G0cnNCVkeHUh?=
HuO-3N1 M4P5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkSzTWM2OD1yLkW0OlU{KM7:TR?= NFqw[nlUSU6JRWK=
RT-112 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHLbGNYUUN3ME2wMlU1PzBzIN88US=> NED0VWJUSU6JRWK=
NEC8 MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLqTWM2OD1yLkW2Nlg6KM7:TR?= NYXPfJRlW0GQR1XS
D-263MG NGKzfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HOWGlEPTB;MD63NVE2QSEQvF2= M4PhfXNCVkeHUh?=
SW962 MlvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofNTWM2OD1yLke4PVg5KM7:TR?= NHqwUm1USU6JRWK=
BV-173 NITBUFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwOES2NlMh|ryP NWjubWxHW0GQR1XS
MFE-280 NWnRfYRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW3TWM2OD1yLki1PFczKM7:TR?= MV\TRW5ITVJ?
HuH-7 NXmyVFBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1OyfGlEPTB;MT6yOFQ3PCEQvF2= NV:0UXl4W0GQR1XS
RS4-11 MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\PUZFKSzVyPUGuN|M5QDZizszN NF;XV5VUSU6JRWK=
DMS-114 NYnuNWVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jRT2lEPTB;MT6zOlc{PyEQvF2= NEjMS2FUSU6JRWK=
MSTO-211H Mk\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV35U41PUUN3ME2xMlQ4Ozd6IN88US=> M3XrPXNCVkeHUh?=
DU-145 NHjUNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDDdnB1UUN3ME2xMlU5OjF5IN88US=> MoPPV2FPT0WU
A172 M1[5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fYemlEPTB;MT63NFM2PSEQvF2= MV3TRW5ITVJ?
SBC-1 NFfjNmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX6XIFlUUN3ME2yMlA6PCEQvF2= MXPTRW5ITVJ?
H9 MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvaTWM2OD1{LkG0N|A3KM7:TR?= MYrTRW5ITVJ?
NCI-SNU-1 NVjw[5BUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH4PG02UUN3ME2yMlE5Ozl2IN88US=> NFnOXFNUSU6JRWK=
NCI-H720 MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7zdmJKSzVyPUKuNlEzQDNizszN M4nhWHNCVkeHUh?=
HCC2218 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJwM{e5N|kh|ryP MkDhV2FPT0WU
G-401 Mof5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfHTWM2OD1{LkS3NVg6KM7:TR?= MmnvV2FPT0WU
MPP-89 MmX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTJwNEizOlQh|ryP MmrkV2FPT0WU
697 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDzbmZKSzVyPUKuOlU{OzFizszN M{PGcnNCVkeHUh?=
KARPAS-45 MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjUdGdKSzVyPUKuO|A4PDdizszN M1vOOXNCVkeHUh?=
MG-63 NVzuSXh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJwOUSyOlIh|ryP NFuxTIpUSU6JRWK=
NTERA-S-cl-D1 NWe2VI83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7GW|hKUUN3ME2zMlA{PDd{IN88US=> NEmxboVUSU6JRWK=
G-402 NUS0O2dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf5Z49KSzVyPUOuNVI4OjdizszN NH7re2VUSU6JRWK=
NKM-1 NHPwbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTNwMUO1OlQh|ryP M1XoU3NCVkeHUh?=
RH-18 Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;nbmlEPTB;Mz6xPVU6QCEQvF2= M{P6dHNCVkeHUh?=
NCI-H1092 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4j2d2lEPTB;Mz6xPVY6KM7:TR?= NYTMXmU6W0GQR1XS
RPMI-8226 NXH0R2hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrhe|RKSzVyPUOuNlM1PDdizszN MUPTRW5ITVJ?
GAMG M2\qXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTNwNE[1O|Yh|ryP MXPTRW5ITVJ?
HH M2rxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXDV4lKSzVyPUOuOFc3PzZizszN M3nuN3NCVkeHUh?=
RO82-W-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1P0[GlEPTB;Mz60PVg2PSEQvF2= MnToV2FPT0WU
CCRF-CEM NW[wPIFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDJeIxmUUN3ME2zMlUxPDh6IN88US=> NEewN5VUSU6JRWK=
NBsusSR MoLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7OXVZOUUN3ME2zMlY{QTZ7IN88US=> MYPTRW5ITVJ?
CHL-1 M1jtXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGn2XppKSzVyPUOuOlU4QTlizszN MVnTRW5ITVJ?
LK-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHK3bGJKSzVyPUOuOlcyOzNizszN Mn;YV2FPT0WU
Hs-578-T NXTQPFVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXETWM2OD1|Lk[3PFc{KM7:TR?= MWjTRW5ITVJ?
CTB-1 M4SwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLPXmlkUUN3ME2zMlgxODVzIN88US=> NVPWT3pxW0GQR1XS
ES5 M2DaU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTlN2M6UUN3ME2zMlg{PjN5IN88US=> MmjqV2FPT0WU
A204 MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fRSGlEPTB;Mz65NlA4PSEQvF2= MY\TRW5ITVJ?
SW780 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTNwOUKyOFUh|ryP NFfPRVRUSU6JRWK=
EW-3 MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1L6NmlEPTB;Mz65PFkzOyEQvF2= NXywRpFbW0GQR1XS
A704 M{nMfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jsXmlEPTB;ND6yPFczOyEQvF2= MWTTRW5ITVJ?
LU-139 M{fFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PIdGlEPTB;ND6zNVU{PCEQvF2= M3j5cnNCVkeHUh?=
CAL-72 NFXqSIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\3TWM2OD12LkSxO|Q3KM7:TR?= NUDwZ5BnW0GQR1XS
D-336MG MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TrZWlEPTB;ND60OlgyPyEQvF2= M4TFOHNCVkeHUh?=
LAMA-84 NWLQR3djT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nEfmlEPTB;ND61N|MyKM7:TR?= MmO3V2FPT0WU
GI-ME-N NES0fWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4O3V2lEPTB;ND61OFgyKM7:TR?= M2\CR3NCVkeHUh?=
KM-H2 M{jqXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7MV3drUUN3ME20MlU2OjJ{IN88US=> MXHTRW5ITVJ?
NCI-H209 NX;xTHpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTRwNUiyPFMh|ryP Mm\OV2FPT0WU
IGROV-1 MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTRwOEexOlgh|ryP NIPBNINUSU6JRWK=
L-363 MlLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXHfGpKSzVyPUSuPVY3PjVizszN MVfTRW5ITVJ?
SK-MEL-3 MoLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL2O2JlUUN3ME21MlI1ODZizszN NFP2O5lUSU6JRWK=
HuO9 Ml;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1uxV2lEPTB;NT6zPFg1OyEQvF2= NH3Zb4lUSU6JRWK=
NOS-1 NUSwbHhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPZTWM2OD13LkeyPVI4KM7:TR?= NVrPV5l{W0GQR1XS
NCI-H1770 NHfPRZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnxTWM2OD13Lkm1NFMzKM7:TR?= NUX0VYZ3W0GQR1XS
SF126 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETGUVFKSzVyPU[uNlE1ODZizszN M{H4fnNCVkeHUh?=
ML-2 M17Efmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTZwMkS5O|ch|ryP MXnTRW5ITVJ?
CHP-134 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nYdGlEPTB;Nj6yOVE5OiEQvF2= M{TE[nNCVkeHUh?=
NCI-H1355 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;MTWM2OD14LkSxO|M{KM7:TR?= NGm2S2pUSU6JRWK=
TE-12 M1Hsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[4d2Z1UUN3ME22MlczPjdzIN88US=> M4Hp[XNCVkeHUh?=
A4-Fuk M3TxVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe5dHVKSzVyPU[uO|MyPDJizszN NWXjcoY{W0GQR1XS
MV-4-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvxZnJKSzVyPU[uO|Y3OjZizszN NUjyWYE3W0GQR1XS
SK-UT-1 NIj1[GRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWX2NJZEUUN3ME22MlkyPzh2IN88US=> M{TsXHNCVkeHUh?=
J-RT3-T3-5 NF3MdYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HQU2lEPTB;Nz6wO|c3PCEQvF2= M3jHXXNCVkeHUh?=
ME-180 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTdwMUC0NFQh|ryP NF7vbHdUSU6JRWK=
SK-MEL-28 M{K5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLNTWM2OD15LkO3PFE6KM7:TR?= NHLFVVdUSU6JRWK=
HAL-01 NHLWS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTGVGpEUUN3ME23MlQ5OzRzIN88US=> M4jDXHNCVkeHUh?=
ES8 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTdwNkm2NlYh|ryP NEPJflZUSU6JRWK=
DB MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nXb2lEPTB;OD6xNVUxPCEQvF2= MmnvV2FPT0WU
SK-NEP-1 NUPpfmttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OyN2lEPTB;OD60PFE1QSEQvF2= MlHJV2FPT0WU
COR-L88 NF6xb3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXWUVlKSzVyPUiuOVA6QDFizszN NG\ENZNUSU6JRWK=
LB1047-RCC M4rjSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRThwNUKyNVIh|ryP MnHiV2FPT0WU
NCI-H520 NF\TUmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRThwNkKxOVch|ryP M1\Ze3NCVkeHUh?=
SW954 MnjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLqTWM2OD16Lk[5O|g3KM7:TR?= MXXTRW5ITVJ?
TE-6 NULDUZdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrhV|VKSzVyPUiuO|UyPDNizszN Ml\ZV2FPT0WU
D-283MED NGjQS|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\MUZRKSzVyPUmuNFY2OzRizszN MVjTRW5ITVJ?
DBTRG-05MG NFnufVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;pTWM2OD17LkC5OlA4KM7:TR?= NV;TbWFsW0GQR1XS
NCI-H446 M3X1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTlwMkm1NlYh|ryP NIH5bmhUSU6JRWK=
HOS NXvs[Ix1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P1T2lEPTB;OT6zOVE{PCEQvF2= NX7wZnh6W0GQR1XS
ES4 NVrJU4FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTlwNUC1PVUh|ryP M{DmfHNCVkeHUh?=
EW-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK1d25KUUN3ME25Mlg6ODV3IN88US=> NIPrR4pUSU6JRWK=
IST-MES1 Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\SR2lEPTB;OT65OFU{PCEQvF2= Mk[5V2FPT0WU
CAS-1 NXz3UphVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTlwOUe2OVkh|ryP M{DGeXNCVkeHUh?=
EM-2 MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFyLkGzPVMh|ryP NYnkToR2W0GQR1XS
SW948 MkHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFyLkG4PFIh|ryP Ml7UV2FPT0WU
OAW-42 M4HSPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDZUGg5UUN3ME2xNE42OjZ5IN88US=> MkiyV2FPT0WU
BE-13 NHziWG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFyLk[1O|Yh|ryP NELTXHlUSU6JRWK=
KU812 Mm[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnrXlBMUUN3ME2xNE44OzlzIN88US=> MY\TRW5ITVJ?
SK-MEL-30 MmHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnKNYN4UUN3ME2xNE45QTBzIN88US=> NWP6OGpzW0GQR1XS
A2780 M1G3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3qSJFKSzVyPUGxMlA{ODhizszN Ml;zV2FPT0WU
TGBC24TKB MnXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLKN5ZTUUN3ME2xNU4xPzN5IN88US=> MnjMV2FPT0WU
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GT3TKB M120XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XwdWlEPTB;NEOuNlY4QSEQvF2= MXfTRW5ITVJ?
RPMI-2650 NFvWdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\VUXpKSzVyPUSzMlc5OTZizszN NX3WOWd7W0GQR1XS
SAS NXy2do9VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7BTWM2OD12Mz65OVM1KM7:TR?= NHz1fHFUSU6JRWK=
MDA-MB-231 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[yTWM2OD12Mz65OlA6KM7:TR?= M1zyZ3NCVkeHUh?=
JVM-3 M2\lPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTR2LkC1N|Mh|ryP NEnGd|BUSU6JRWK=
COLO-320-HSR NXzjenhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjPWVVKSzVyPUS0MlU3OzNizszN NG\LTZRUSU6JRWK=
SNB75 NU\ZV4ZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTR2Lk[xNFUh|ryP NGj4XXdUSU6JRWK=
NCI-H441 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDuVod7UUN3ME20OE46OzJ6IN88US=> M3ztXXNCVkeHUh?=
HCT-116 M4P2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;6RWFzUUN3ME20OE46QDZ6IN88US=> NYr5SopOW0GQR1XS
NCI-H226 NVnMU2kzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzsTWM2OD12NT62N|Y5KM7:TR?= NWKwSlR[W0GQR1XS
CAL-33 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrYNG1{UUN3ME20OU46OjF5IN88US=> NFvuZ5FUSU6JRWK=
NCI-H1437 M1XMTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\nSlVKSzVyPUS2MlMzOSEQvF2= MorSV2FPT0WU
HCC1187 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTR4LkSyOVUh|ryP NFH1Z|lUSU6JRWK=
NUGC-3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fqRWlEPTB;NE[uOVcxQSEQvF2= M4n4V3NCVkeHUh?=
T98G NYridnl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jMOWlEPTB;NEeuOVQ4KM7:TR?= MoTVV2FPT0WU
OVCAR-8 M1vCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7W[WhKSzVyPUS3MlY5OyEQvF2= NFu2U4ZUSU6JRWK=
LB2241-RCC NIq3ZnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq3TWM2OD12Nz63Nlch|ryP MVPTRW5ITVJ?
NCI-H358 M{TROmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTjTWM2OD12OD6xNVUzKM7:TR?= M4[yeHNCVkeHUh?=
PANC-08-13 NGXQeYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnyxTWM2OD12OD6xPFU{KM7:TR?= MVvTRW5ITVJ?
KP-N-YN MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Ln[mlEPTB;NEiuNlExOiEQvF2= M1rTUnNCVkeHUh?=
NCI-H1755 NYS4dIJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHlfFVKSzVyPUS4MlI4OjZizszN MYnTRW5ITVJ?
NCI-N87 NF23SVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTR6LkK5PVEh|ryP MXvTRW5ITVJ?

... 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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  • Computed Result

  • C1=C0/X C1: LOG(C1):
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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

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