Name: Lifirafenib HCl
Rating: 5 (10 reviews)

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HIT ID:HIT220913476
Cas No:2025320-97-0
常用名:Lifirafenib HCl
IUPAC:5-{[(2R,3R,4S)-3-[6-(trifluoromethyl)-1H-1,3-benzodiazol-2-yl]-5-oxatricyclo[4.4.0.0^{2,4}]deca-1(10),6,8-trien-9-yl]oxy}-2,3,4,8-tetrahydro-1,8-naphthyridin-2-one hydrochloride
IUPAC:5-{[(2R,3R,4S)-3-[6-(trifluoromethyl)-1H-1,3-benzodiazol-2-yl]-5-oxatricyclo[4.4.0.0^{2,4}]deca-1(10),6,8-trien-9-yl]oxy}-2,3,4,8-tetrahydro-1,8-naphthyridin-2-one hydrochloride
InChI key:InChIKey=QJAXJBSVURJFCX-SGIIKHNDSA-N

分子式:C25H18ClF3N4O3
分子量:514.89
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
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
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

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.

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