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AS-703026
品牌: Adipogen
产品货号: SYN-1190-M001
规格: 1 mg

报价:
折后价:

数量: - +
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.
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  • 保存温度:
    +4°C
  • 运输温度:
    AMBIENT
  • 细胞定位:
  • 预期分子量:
    431.2
  • 产品形式:
    solid
  • 存储溶液:
  • 有效期:
    Stable for at least 1 year after receipt when stored at +4°C.
  • 产地:
    瑞士
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  • 纯度:
    >95%
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  • CAS号:
    1236699-92-5
  • 分子式:
    C15H15FIN3O3
  • 溶解度:
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