|
MCE 国际站:Selinexor
CAS:1393477-72-9
品牌:MedChemExpress (MCE)
存储条件:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
生物活性:Selinexor (KPT-330),是 KPT-185 的类似物。Selinexor 是一种口服有效的、选择性的 CRM1 抑制剂。
体外:作为 KPT-185 的临床候选类似物,KPT-330 对 T-ALL 细胞的活力表现出相似的作用,并引发快速的细胞凋亡反应。KPT-330 还减少 MOLT-4、Jurkat、HBP-ALL、KOPTK-1、SKW-3 和 DND-41 细胞系的细胞生长,IC50 值为 34-203 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内:Selinexor (KPT-330) 在体内显著抑制 T-ALL 细胞 (MOLT-4) 和 AML 细胞 (MV4-11) 的生长,对正常造血细胞几乎没有毒性[1]。 在具有弥漫性人类 MM 骨损伤的 SCID 小鼠中,KPT-330 抑制 MM 诱导的骨溶解并延长存活期。此外,KPT-330 通过阻断 RANKL 诱导的 NF-κB 和 NFATc1 直接损害破骨细胞生成和骨吸收,对成骨细胞和 BMSCs 的影响最小[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Clinical Trial
热销产品:Cellulase | Saikosaponin C | Velpatasvir | Vistusertib | | | | | |
研究领域:Membrane Transporter/Ion Channel
作用靶点:CRM1
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr;161(1):117-27.
[2]. Tai YT, et al. CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications. Leukemia. 2014 Jan;28(1):155-65.
Archiver|手机版|科学网 ( 京ICP备07017567号-12 )
GMT+8, 2024-8-7 08:26
Powered by ScienceNet.cn
Copyright © 2007- 中国科学报社