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Selinexor

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Chemical Structure| 1393477-72-9 同义名 : KPT-330;ATG-010
CAS号 : 1393477-72-9
货号 : A140158
分子式 : C17H11F6N7O
纯度 : 99%+
分子量 : 443.306
MDL号 : MFCD27987944
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(112.79 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 13 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • CRM1
描述 Chromosome region maintenance 1 (CRM1) is a major nuclear export receptor that mediates the transport of proteins and mRNAs. KPT-330 is a selective inhibitor of CRM1 which shows cytotoxic activity with a median IC50 value of 123 nM in a characterized cell penal with 23 cell lines[1]. In both STO and MesoII cells, the treatment of 1 μM KPT-330 markedly increased the accumulation of G1phase at 48 hours after the exposure, and reached a maximum at 72 hours. STO cells demonstrated a high sensitivity to KPT-330 with an IC50 of 0.7 μM, whereas MesoII cells with IC50 of 0.35 μM[2]. KPT-330 at the concentration between 0.1 μM–1 μM induced growth inhibition dose-dependently in eleven NSCLC cell lines. KPT-330 at 1 μM also stimulated the activation of caspase-3 and caspase-9, as well as the protein levels of several pro-apoptotic mediators, including Bax, Bim, and Puma in NSCLC cells. When evaluating the tumor volume of H1975 NSCLC cells engrafted in NOD/SCID mice, KPT-330 treatment (10 mg/kg, twice weekly for 4 weeks) markedly inhibited tumor growth compared with vehicle-treated controls[3].
作用机制 KPT-330 inactivates CRM1 by modifying the critical CRM1-binding residue, thereby irreversibly inhibiting CRM1-mediated nuclear export of proteins and mRNAs[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.28mL

2.26mL

1.13mL

22.56mL

4.51mL

2.26mL
参考文献

[1]Attiyeh EF, Maris JM, et al. Pharmacodynamic and genomic markers associated with response to the XPO1/CRM1 inhibitor selinexor (KPT-330): A report from the pediatric preclinical testing program. Pediatr Blood Cancer. 2016;63(2):276-86.

[2]De Cesare M, Cominetti D, et al. Anti-tumor activity of selective inhibitors of XPO1/CRM1-mediated nuclear export in diffuse malignant peritoneal mesothelioma: the role of survivin. Oncotarget. 2015;6(15):13119-32.

[3]Sun H, Hattori N, et al. KPT-330 has antitumour activity against non-small cell lung cancer. Br J Cancer. 2014;111(2):281-91.

[4]https://pubchem.ncbi.nlm.nih.gov/compound/Selinexor#section=Top