产品说明书

Verdinexor

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Chemical Structure| 1392136-43-4 同义名 : KPT-335;ATG-527
CAS号 : 1392136-43-4
货号 : A209806
分子式 : C18H12F6N6O
纯度 : 99%+
分子量 : 442.318
MDL号 : MFCD28167840
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(237.39 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 8 mg/mL clear

PO 0.5% CMC-Na 70 mg/mL suspension

生物活性
靶点

  • CRM1
描述 Verdinexor (KPT-335) is an innovative, orally-administered selective inhibitor of nuclear export (SINE) that blocks the nuclear export protein Exportin 1 (XPO1/CRM1), showing efficacy against canine cancer cell lines[1]. KPT-335 effectively hinders cell proliferation, prevents colony formation, and triggers cell apoptosis at doses that are biologically significant. It also leads to a decrease in XPO1 protein levels alongside an increase in XPO1 mRNA levels. Additionally, treatment with KPT-335 elevates the expression and nuclear presence of the tumor suppressor proteins p53 and p21[3]. Prophylactic and therapeutic use of verdinexor offers protection to mice from influenza virus strains A/California/04/09 and A/Philippines/2/82-X79, lowering lung viral counts and inflammatory cytokine levels while showing minimal toxicity[1]. The inhibition of XPO1 by KPT-335 also curtails cyst growth in vivo in the Pkd1 mutant mouse model Pkd1v/v[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.30mL

2.26mL

1.13mL

22.61mL

4.52mL

2.26mL
参考文献

[1]Munuce MJ, et al. Effects of ulipristal acetate on sperm DNA fragmentation during in vitro incubation. Eur J Contracept Reprod Health Care. 2013 Oct;18(5):355-63.

[2]Pohl O, et al. A 39-week oral toxicity study of ulipristal acetate in cynomolgus monkeys. Regul Toxicol Pharmacol. 2013 Jun;66(1):6-12.

[3]Attardi BJ, et al. In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88.