BGB-283 is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively. BGB-283 potently inhibits BRafV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRafV600E and EGFR mutation/amplification. In BRafV600E colorectal cancer cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. 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 BRafV600E mutation.

Product information

CAS Number: 1446090-77-2

Molecular Weight: 478.42

Formula: C25H17F3N4O3

Chemical Name: 5-{[(2R,3R,4S)-3-[6-(trifluoromethyl)-1H-1,3-benzodiazol-2-yl]-5-oxatricyclo[4.4.0.0²,⁴]deca-1(6),7,9-trien-9-yl]oxy}-1,2,3,4-tetrahydro-1,8-naphthyridin-2-one

Smiles: O=C1CCC2C(NC=CC=2OC2=CC3[C@@H]4[C@H](OC=3C=C2)[C@H]4C2NC3=CC(=CC=C3N=2)C(F)(F)F)=N1 |&1:14,15,20|

InChiKey: NGFFVZQXSRKHBM-FKBYEOEOSA-N

InChi: InChI=1S/C25H17F3N4O3/c26-25(27,28)11-1-4-15-16(9-11)31-24(30-15)21-20-14-10-12(2-5-17(14)35-22(20)21)34-18-7-8-29-23-13(18)3-6-19(33)32-23/h1-2,4-5,7-10,20-22H,3,6H2,(H,30,31)(H,29,32,33)/t20-,21-,22-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.