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BLU9931

Chemical Structure : BLU9931

CAS No.: 1538604-68-0

BLU9931 (BLU-9931)

Catalog No.: PC-43232Not For Human Use, Lab Use Only.

BLU9931 (BLU-9931) is a potent, selective, irreversible inhibitor of FGFR4 with IC50 of 3 nM, shows much weaker activity for FGFR1 (IC50=591 nM), FGFR2 (IC50=493 nM) and FGFR3 (IC50=150 nM).

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Biological Activity

BLU9931 (BLU-9931) is a potent, selective, irreversible inhibitor of FGFR4 with IC50 of 3 nM.
BLU9931 shows much weaker activity for FGFR1 (IC50=591 nM), FGFR2 (IC50=493 nM) and FGFR3 (IC50=150 nM).
BLU9931 potently and selectively inhibits FGFR4 signaling and cell proliferation in HCC cell lines with an activated FGFR4 signaling pathway (Huh-7 cell IC50=110 nM, JHH-7 IC50=20 nM).
BLU9931 shows remarkable antitumor activity in mice bearing HCC tumor xenograft that overexpresses FGF19.

Physicochemical Properties

M.Wt 509.3839
Formula C26H22Cl2N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 17 mg/mL

Chemical Name/SMILES

2-Propenamide, N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-

References

1. Hagel M, et al. Cancer Discov. 2015 Apr;5(4):424-37.

2. Packer LM, et al. Cancer Discov. 2015 Apr;5(4):355-7.

3. Yamamoto M, et al. Cancer Sci. 2018 Mar 13. doi: 10.1111/cas.13569.

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