AS-703026-其他小分子化合物-深圳欣博盛生物科技有限公司

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AS-703026

品牌：Adipogen

官网链接

说明书

折扣/货期

货号：SYN-1190-M001	规格：1 mg	目录价：￥910
货号：SYN-1190-M005	规格：5 mg	目录价：￥1358
货号：SYN-1190-M010	规格：10 mg	目录价：￥1820
货号：SYN-1190-M050	规格：50 mg	目录价：￥5894
货号：SYN-1190-M100	规格：100 mg	目录价：￥询价

产品详情

* 以下信息仅供参考，详情请以原厂网站为准

产品名称:

AS-703026

别名:

AS703026

产品描述:

AS703026 is a novel, selective, non-competitive, orally bioavailable MEK1/2 inhibitor with experimental IC(50) values of 5-11nM. In use on multiple myeloma cells (MM), AS703026 inhibited growth and survival of MM cells and cytokine-induced osteoclast differentiation more potently (~10X) 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. AS703026 further induced apoptosis via caspase 3 and Poly ADP ribose polymerase (PARP) cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs). Importantly, AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. Significant tumour growth reduction in AS703026- vs. vehicle-treated mice bearing H929 MM xenograft tumours correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels in vivo. Moreover, AS703026 (< 200nM) was cytotoxic against the majority of tumour cells tested from patients with relapsed and refractory MM (84%), regardless of mutational status of RAS and BRAF genes. Importantly, BMSC-induced viability of MM patient cells was similarly blocked within the same dose range.

保存温度:

+4°C

运输温度:

Ambient

预期分子量:

431.2

产品形式:

solid

产地:

瑞士

纯度:

>95%