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Trametinib(DMSO solvate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Trametinib(DMSO solvate)图片
CAS NO:1187431-43-1
包装与价格:
包装价格(元)
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
GSK-1120212 (DMSO solvate)
Trametinib dimethyl sulfoxide
JTP-74057 (DMSO solvate)
Trametinib DMSO solvate
产品介绍
Trametinib (DMSO solvate)是一种口服有效的MEK抑制剂,抑制 MEK1 和 MEK2 的IC50分别为 2 nM。它还能激活自噬,诱导凋亡。

产品描述

Trametinib DMSO solvate is a Highly Potent and Selective MEK Inhibitor that specifically inhibits MEK1/2(IC50 :2 nM)

体外活性

Trametinib DMSO solvate displays remarkable potency in cellular assays for ERK1/2 phosphorylation and growth inhibition and excellent in vivo activity.?Inhibition of the MEK?ERK pathway offers a very promising therapeutic strategy for cancers with activating mutant Ras and Raf, and GSK1120212 (DMSO solvate) has been advanced into phase III trials for advanced or metastatic BRAF mutant melanoma as well as phase I and II studies in subjects with solid tumors or leukemia.

体内活性

Trametinib DMSO solvate was then evaluated in vivo in an A549 (KRAS mutant cell line) xenograft model, orally dosing daily for 21 days (qd × 21).Near complete tumor growth inhibition was observed at 5.0 and 2.5 mg/kg [92 and 87% tumor growth inhibition (TGI), respectively] and to a lesser degree at 0.5 and 0.1 mg/kg (62 and 58% TGI).?[Notably, although 5 mg/kg was the maximally tolerated dose (MTD) , 3 mg/kg is the typically observed MTD.] Dose-dependent antitumor activity with GSK1120212 (DMSO solvate) treatment has been similarly reported for several other KRAS and BRAF mutant tumor models.

Cas No.

1187431-43-1

分子式

C28H29FIN5O5S

分子量

693.53

别名

GSK-1120212 (DMSO solvate);Trametinib dimethyl sulfoxide;JTP-74057 (DMSO solvate);Trametinib DMSO solvate

储存和溶解度

DMSO:69 mg/mL (99.49 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years