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KPT-276
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KPT-276图片
CAS NO:1421919-75-6
规格:98%
分子量:426.26
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
inhibitor of nuclear export (SINE) and CRM1, orally bioavailable
CAS:1421919-75-6
分子式:C16H10F8N4O
分子量:426.26
纯度:98%
存储:Store at -20°C

Background:

KPT-276, analog of KPT-185, is a selective inhibitor of nuclear export (SINE) and CRM1 [1].


Chromosomemaintenance protein 1 (CRM1) is a nuclear export receptor involved in the active transport of transcription factors, cell-cycle regulators, tumor suppressors and RNA molecules. In cancer, CRM1 is overexpression and overactive transport [1].


KPT-276 is an orally bioavailable and selective CRM1 inhibitor that irreversibly binds to CRM1 and blocks CRM1-mediated nuclear export [1]. In human multiple myeloma (MM) cell lines (HMCLs), KPT-276 irreversibly and specifically inhibited the nuclear export of XPO1, which encoded CRM1 and significantly reduced the viability of HMCLs. In bone marrow cells isolated from MM patients, KPT-276 induced apoptosis. Also, KPT-276 downregulated the expression of c-MYC, CDC25A and BRD4, which caused G1/S phase arrest [2].


In a xenograft human acute myeloid leukemia (AML) murine model, KPT-276 significantly increased the survival of mice and reduced the amount of white blood cells. Also, KPT-276 significantly reduced spleen weight and FLT3 protein expression [1]. In a xenograft MM mouse model, KPT-276 inhibited tumor growth [2].


参考文献:
[1].  Ranganathan P, Yu X, Na C, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood, 2012, 120(9): 1765-1773.
[2].  Schmidt J, Braggio E, Kortuem KM, et al. Genome-wide studies in multiple myeloma identify XPO1/CRM1 as a critical target validated using the selective nuclear export inhibitor KPT-276. Leukemia, 2013, 27(12): 2357-2365.