>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

Trametinib (GSK1120212)

Trametinib (GSK1120212) 曲美替尼; GSK1120212; JTP-74057

Trametinib (GSK1120212, JTP-74057)是一种高特异性的，有效的MEK1/2抑制剂，无细胞试验中IC50为0.92 nM/1.8 nM，对c-Raf， B-Raf， ERK1/2没有抑制活性。Trametinib 可激活自噬并诱导凋亡。

货号：
TK0168
规格：

10mg

25mg

50mg
价格：
￥0.00

产品参数

CAS No.	871700-17-3
生物活性	Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
分子式	C26H23FIn5O4
分子量	615.39
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 25 mg/mL (40.62 mM; ultrasonic and warming and heat to 60°C)
体内研究	Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of Trametinib (GSK1120212; JTP-74057) or 10 mg/kg of HWA486. Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) is effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model.
体外研究	Trametinib (GSK1120212;JTP-74057) (0.1-100 nM) blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs). Trametinib (JTP-74057) inhibits the growth of 9 out of 10 human colorectal cancer cell lines, and they shows cell-cycle arrest at the G1 phase after drug tratment. The combination of GSK2118436 and Trametinib (GSK1120212) effectively inhibits cell growth, decreases ERK phosphorylation, decreases cyclin D1 protein, and increases p27(kip1) protein in the resistant clones.
文献	暂无相关参考文献
纯度及产品资料	98%

推荐产品