BGB-283

SKU: C-1078-5mg

Quantity (mg):

5 mg

Product Options

Quantity

$103.99

Catalog#: C-1078

Targets: RAF, EGFR

Synonym: BGB-283; BGB 283; BGB283

Chemical Name/IUPAC:5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-5-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one

SMILES Code: [H][C@@]1(C2=CC(OC3=C(CCC4=O)C(N4)=NC=C3)=CC=C2O[C@]51[H])[C@@H]5C6=NC7=CC=C(C=C7N6)C(F)(F)F

Technical Data

Product Name: BGB-283

Chemical Formula: C25H17F3N4O3

Molecular Weight: 478.43

CAS#: 1446090-77-2

Appearance: Solid powder

Purity: > 99% by HPLC

Solubility: Soluble in DMSO

Storage: Room temperature for months, or -20ºC for 3 years

Description
BGB-283 is a 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.

BGB-283

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