现货,AS703026,CAS号:1236699-92-5,美国进口, MAPK ,MEK , MEK 抑制剂和化合物,selleck,S1475

信号转导通路: MAPK >> MEK >> MEK 抑制剂 >> AS703026http://www.selleck.cn/as703026-S1475.html

技术数据:

分子量(MW): 431.20

化学式: C15H15FIN3O3

溶解度: DMSO ≥86mg/mL Water <1mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1236699-92-5

 

生物活性

 

AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor, in human multiple myeloma (MM). AS703026 inhibited growth and survival of MM cells (cell IC50 ranging from 0.005 to 2 μM) and cytokine-induced osteoclast differentiation more potently (9- to 10-fold) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression.

Importantly, AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. [1]

 

参考文献

Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Kim K, et al. Br J Haematol. 2010 May;149(4):537-49.

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