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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
有效期:
Stable for at least 1 year after receipt when stored at +4°C.
产地:
瑞士
纯度:
>95%
CAS号:
1236699-92-5
分子式:
C15H15FIN3O3
溶解度:
Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.
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