BLU-554

Research use only, not for human use.

BLU-554 (Fisogatinib, BLU554) is a novel potent, highly selective and orally bioavailable inhibitor of FGFR4 designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation.

BLU-554 (Fisogatinib, BLU554) is a novel potent, highly selective and orally bioavailable inhibitor of FGFR4 designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation; targets FGFR4 while sparing other members of the FGFR family and showing little to no inhibition of all other kinases.Liver Cancer Phase 1 Clinical(In Vivo):Tissue distribution of Fisogatinib (10?mg/kg; oral gavage; for 4 hours; FVB/NRj mice) in wild-type mice is as follows; tissue concentrations decreases in the order liver?>?kidney?>?small intestine?>?spleen?>?brain. The high Fisogatinib liver-to-plasma ratio suggests there is a relatively high amount of the drug being transported into the liver.

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Tissue distribution of Fisogatinib (10 mg/kg; oral gavage; for 4 hours; FVB/NRj mice) in wild-type mice is as follows; tissue concentrations decreases in the order liver > kidney > small intestine > spleen > brain. The high Fisogatinib liver-to-plasma ratio suggests there is a relatively high amount of the drug being transported into the liver. Animal Model:Wild type male mice(FVB/NRj, 11-14?weeks of age)Dosage:10?mg/kg Administration:Oral gavage; for 4 hours (Pharmacokinetic study)Result:Tissue concentrations decreased in the order liver?>?kidney?>?small intestine?>?spleen?>?brain.

Fisogatinib | BLU554

Angiogenesis

FGFR

FGFR1|FGFR2|FGFR3|FGFR4

Cancer

Liver Cancer

1707289-21-1

503.3777

C24H24Cl2N4O4

>98% (HPLC)

DMSO: ≥ 25 mg/mL

COC1=CC(=C(C(=C1Cl)C2=CC3=CN=C(N=C3C=C2)NC4COCCC4NC(=O)C=C)Cl)OC

2-Propenamide, N-[(3S,4S)-3-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]tetrahydro-2H-pyran-4-yl]-

(-20℃)

With Ice Pack

≥ 2 years