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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Exportin-1 (CRM1,XPO1)-CBS9106
CBS9106

Chemical Structure : CBS9106

CAS No.: 1076235-04-5

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CBS9106 (Felezonexor, SL-801)

货号: PC-23458Not For Human Use, Lab Use Only.

CBS9106 (Felezonexor) is a reversible oral CRM1/exportin1 inhibitor, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a broad spectrum of cancer cells.

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2 mg ￥2580 In stock
5 mg ￥4280 In stock
10 mg ￥7280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CBS9106 (Felezonexor) is a reversible oral CRM1/exportin1 inhibitor, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a broad spectrum of cancer cells.
CBS9106 (Felezonexor) sensitize cells to radiation and to suppress the growth of a variety of cancer cell lines with IC50 values ranged from 22.3 or 35.6 nM in MM.1S or RPMI-8226 cells and from 3 to 278 nM in 60 other human cancer cell lines.
CBS9106 (Felezonexor) inhibits HIV Rev function with IC50 of 5.5 nM.
CBS9106 decreases CRM1 protein expression levels in MM.1S cells, inhibits NF-κB activity by protection against IκB-α degradation.
CBS9106-mediated CRM1 depletion requires ubiquitin/proteasome pathway.
CBS9106 directly binds to CRM1 in a competitive manner with Leptomycin B, binds Cys528 of CRM1 and the binding is reversible.
CBS9106 (Felezonexor) significantly suppresses tumor growth and prolongs survival in human MM xenograft models.

物理化学性质&存储条件

分子量 419.83
分子式 C18H21ClF3N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-((6-Chloro-5-(trifluoromethyl)pyridin-2-yl)amino)-3-((3,3-dimethylbutoxy)methyl)-4-methyl-1H-pyrrole-2,5-dione

参考文献

1. Saito N, et al. Mol Cancer Ther. 2014 Dec;13(12):3013-23.

2. Sakakibara K, et al. Blood. 2011 Oct 6;118(14):3922-31.

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