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抑制剂/激活剂

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凋亡与自噬

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Dabrafenib 达拉非尼; GSK2118436A; GSK2118436

Dabrafenib是一种突变型BRAFV600E特异性抑制剂，无细胞试验中IC50为0.7 nM，作用于B-Raf(wt)和c-Raf效果分别低7和9倍。

货号：
TK0385
规格：

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	1195765-45-7
生物活性	Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf, respectively.
分子式	C23H20F3N5O2S2
分子量	519.56
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 33 mg/mL (63.52 mM)
体内研究	Dabrafenib-treated females have mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females have keratinized and histologically open vaginas.
体外研究	Dabrafenib (GSK2118436, 1 μM) with 0.01 μM GSK1120212 inhibits more than 90% of cell growth in the NRAS mutant clones. GSK2118436 is sufficient to reduce S6P phosphorylation in A375. Dabrafenib suppresses the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6. Dabrafenib inhibits the release of HMGB1 and downregulates HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells.
纯度及产品资料	98%

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