BGB-283|1446090-77-2--Shanghai xingMo Biotechnology

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Description

BGB-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.

Chemical Structure

Chemical Name

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

Theoretical Analysis

XingMo Cat#:XM156
Product Name:BGB-283
Synonyms:BGB-283; BGB 283; BGB283.
CAS#:1446090-77-2
Chemical Formula:C₂₅H₁₇F₃N₄O₃
Exact Mass:478.12528
Molecular Weight:478.43

Technical Data

Appearance: solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).

WARNING: This product is for research use only, not for human or veterinary use

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