BLU-9931

  Cat. No.:  DC8280   Featured
Chemical Structure
1538604-68-0
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More than 5000 active chemicals with high quality for research!
Field of application
BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM).
Cas No.: 1538604-68-0
Chemical Name: N-[2-[[6-(2,6-Dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-3-methylphenyl]prop-2-enamide
Synonyms: Blu9931;Blu-9931;BLU 9931;FQK825B5DX;N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-3-methylphenyl]prop-2-enamide;N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide;GTPL8862;BCP15296;s7819;BDBM50233461;SB19004;AK318441;N-(2-((6-(2,6-Dichloro-3,5-dimethoxyphenyl)-2-quinazoli
SMILES: ClC1C(=C([H])C(=C(C=1C1C([H])=C([H])C2C(=C([H])N=C(N=2)N([H])C2C(=C([H])C([H])=C([H])C=2C([H])([H])[H])N([H])C(C([H])=C([H])[H])=O)C=1[H])Cl)OC([H])([H])[H])OC([H])([H])[H]
Formula: C26H22Cl2N4O3
M.Wt: 509.3839
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with an IC50 of 3 nM.
In Vivo: BLU9931 (300 mg/kg, p.o.) leads to tumor regression and prevents this weight loss in mice bearing the FGF19-amplified Hep 3B liver tumors. In mice bearing the FGF19-overexpressing PDX-derived LIXC012 xenografts, treatment with BLU9931 (300 mg/kg, p.o.) also leads to tumor regression[1].
In Vitro: In MDA-MB-453 cells, BLU9931 potently inhibits phosphorylation of FGFR4 signaling pathway. BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, such as Hep 3B, HUH-7, and JHH-7 cell lines, with EC50 of <1 μM. BLU9931 also inhibits proliferation in PDX-derived cell lines with an intact FGFR4 signaling pathway[1]. BLU9931 induces tumor shrinkage in hepatocellular carcinoma models that express a functioning ligand/receptor complex consisting of FGF19/FGFR4/KLB and adds to a growing list of anti-FGFR4 agents[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC8280 BLU-9931 BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM).
DC1075 AZD4547 AZD4547 is a novel selective FGFR inhibitor targeting FGFR1, FGFR2, and FGFR3 with IC50 of of 0.2 nM, 2.5 nM, and 1.8 nM, respectively.
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