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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-Dabrafenib
Dabrafenib

Chemical Structure : Dabrafenib

CAS No.: 1195765-45-7

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Dabrafenib (GSK2118436A, GSK2118436)

货号: PC-24572Not For Human Use, Lab Use Only.

Dabrafenib (GSK2118436) is potent, selective ATP-competitive inhibitor of Raf with IC50 of 5 nM and 0.6 nM for C-Raf and B-Raf V600E respectively, also potently inhibits RIPK3 with IC50 of 28 nM.

规格 价格 库存 数量
10 mg ￥580 In stock
25 mg ￥880 In stock
50 mg ￥1280 In stock
100 mg ￥1980 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Dabrafenib (GSK2118436) is potent, selective ATP-competitive inhibitor of Raf with IC50 of 5 nM and 0.6 nM for C-Raf and B-Raf V600E respectively, also potently inhibits RIPK3 with IC50 of 28 nM.
Dabrafenib displayed highly selective inhibition on RIP3 over RIP1, RIP2 and RIP5.
Dabrafenib rescued cells from RIP3-mediated necroptosis induced by the necroptosis-induced combinations, that is, tumor necrosis factor (TNF)α, TNF-related apoptosis-inducing ligand or Fas ligand plus Smac mimetic and the caspase inhibitor z-VAD.
Dabrafenib decreased the RIP3-mediated Ser358 phosphorylation of mixed lineage kinase domain-like protein (MLKL) and disrupted the interaction between RIP3 and MLKL.

物理化学性质&存储条件

分子量 519.56
分子式 C23H20F3N5O2S2
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

10 mM in DMSO
Chemical Name/SMILES

N-(3-(5-(2-Aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide

参考文献

1. Hong DS, et al. Clin Cancer Res. 2012 Apr 15;18(8):2326-35.

2. Falchook GS, et al. Lancet. 2012 May 19;379(9829):1893-901.

3. Greger JG, et al. Mol Cancer Ther. 2012 Apr;11(4):909-20.

4. Li JX, et al. Cell Death Dis. 2014 Jun 5;5(6):e1278.

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