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| 产品描述 |
| 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. |
| 化学结构 |
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| 化学名称 |
| 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 |
| 基本信息 |
产品编号:XM156
产品名称:BGB-283
别名:BGB-283; BGB 283; BGB283.
CAS#:1446090-77-2
分子式:C25H17F3N4O3
精确分子量:478.12528
分子量:478.43
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| 物化性质 |
外观: 固体粉末
纯度: >98%
运输信息: 非危险化学品，适于常温或冰袋运输。
储存条件: 低温，干燥，避光。
溶解性: 溶于DMSO, 不溶于水
储存期限:3年 -20℃固体储存
2 年 -80℃ 溶液储存 |
该产品只供科研使用，不能给病人提供。
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