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]. |