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KPT-276 结构式

KPT-276

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货号 :BCP09428CAS号 :1421919-75-6纯度:98%
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  • 基本信息与产品描述
CAS号 1421919-75-6 货号 BCP09428
中文名 KPT-276
英文名 KPT-276
中文别名
英文别名 KPT 276;KPT276;
SMILES C1C(CN1C(=O)C=CN2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)(F)F
化学名称
分子式 C16H10F8N4O 分子量 426.26
纯度 98% 配送 惯例下常温包邮
产品描述 KPT-276, analog of KPT-185, is an orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of CRM1. IC50 value: Target: CRM1 in vitro: A selective inhibitor of nuclear export compound KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1. The viability of 12 HMCLs treated with KTP-276 was significantly reduced. KPT-276 also actively induced apoptosis in primary MM patient samples. In gene expression analyses, two genes of probable relevance were dysregulated by KPT-276: cell division cycle 25 homolog A (CDC25A) and bromodomain-containing protein 4 (BRD4), both of which are associated with c-MYC pathway . Inhibition of CRM1 by two novel selective inhibitors of nuclear export (SINE), KPT-185 and KPT-276, in MCL cells resulted in significant growth inhibition and apoptosis induction. KPT-185 also induced CRM1 accumulation in the nucleus, resulting in CRM1 degradation by the proteasome .
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