Trametinib (GSK1120212)

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价格

促销价

数量
25mg

￥438.00

350.00

- +
50mg

￥625.00

500.00

- +
100mg

￥1000.00

800.00

- +
250mg

￥1750.00

1400.00

- +
500mg

￥2750.00

2200.00

- +

已选 0 种 0 瓶

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MEK1 and MEK2 inhibitor, potent and selective

货号：ajci11258
CAS：871700-17-3
分子式：C26H23FIN5O4
分子量：615.39
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. It has demonstrated broad antitumor activities in a variety of tumor xgenograft models, including HT-29 and COLO205 colorectal tumor cell lines. Trametinib induces expression of p15 and p27, reduces cyclin D1 levels, and causes dephosphorylation of RB protein and G1-phase arrest with a reduction of TS expression in HT-29 cells. It also effectively inhibits p-ERK 1/2 resulting in cell growth inhibition in tumor cell lines harboring B-RAF mutant.

Reference

[1].Akintunde Akinleye, Muhammad Furqan, Nikhil Mukhi, Pavan Ravella and Delong Liu. MEK and the inhibitors: from bench to bedside. Journal of Hematology & Oncology 2013, 6:27
[2].Motoki Watanabe, Yoshihiro Sowa, Mayumi Yogosawa and Toshiyuki Sakai. Novel MEK inhibitor trametinib and other retinoblastoma gene (RB)-reactivating agents enhance efficacy of 5-fluorouracil on human colon cancer cells. Cancer Sci 2013; 104(6): 687-693