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Catalog Number | orb1739495 |
---|---|
Category | Small Molecules |
Description | Lifirafenib HCl |
CAS Number | 2025320-97-0 |
Purity | 0.98 |
MW | 513.9012 |
SMILES | Cl.[H][C@]12Oc3ccc(OC4=C5CCC(=O)N=C5NC=C4)cc3[C@@]1([H])[C@@H]2c1nc2ccc(cc2[nH]1)C(F)(F)F |
Formula | C26H19ClF3N3O3 |
Biological Activity | Lifirafenib, also known as Beigene-283, is a Novel potent and selective RAF Kinase and EGFR inhibitor. BGB-283-displays Potent Antitumor Activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 potently inhibits B-RAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harbouring B-RAFV600E and EGFR mutation/amplification. In B-RAFV600E CRC cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. In vivo, BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell-line derived and primary human colorectal tumor xenografts bearing B-RAFV600E mutation. BGB-283 as a potent antitumor drug candidate with clinical potential for treating CRC harbouring B-RAFV600E mutation. |
Storage | -20°C |
Note | For research use only |
Expiration Date | 12 months from date of receipt. |