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BGB-283

Chemical Structure : BGB-283

CAS No.: 1446090-79-4

BGB-283 (Lifirafenib;BGB 283;BGB283)

货号: PC-45573Not For Human Use, Lab Use Only.

BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM).
BGB-283 (Lifirafenib) inhibits recombinant BRAFV600E with IC50 of 23 nM; also inhibits EGFR and EGFR T790M/L858R with IC50 of 29 nM and 495 nM respectively.
BGB-283 (Lifirafenib) potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation in vitro.
BGB-283 (Lifirafenib) shows tumor growth inhibition in both cell line-derived and primary human colorectal tumor xenografts bearing BRAF(V600E) mutation.

物理化学性质&存储条件

分子量 478.43
分子式 C25H17F3N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 125 mg/mL

Chemical Name/SMILES

5-[[(1R,1aS,6bR)-1a,6b-Dihydro-1-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1H-cyclopropa[b]benzofuran-5-yl]oxy]-3,4-dihydro-1,8-naphthyridin-2(1H)-one

参考文献

1. Tang Z, et al. Mol Cancer Ther. 2015 Oct;14(10):2187-97.

2. Cancer Discov. 2016 Jul;6(7):OF1.

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