Selinexor-KPT-330-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESelinexorCat. No.: HY-17536CAS No.: 1393477-72-9Synonyms: KPT-330分式: CHFNO分量: 443.31作靶點(diǎn): CRM1作通路: Membrane Transporter/Ion Channel儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 48 mg/mL (1

2、08.28 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2558 mL 11.2788 mL 22.5576 mL5 mM 0.4512 mL 2.2558 mL 4.5115 mL10 mM 0.2256 mL 1.1279 mL 2.2558 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Selinexor (KPT-330)，KPT-185 的類似物，

3、 種服活性的，CRM1 的選擇性抑制劑。IC50 & Target CRM1體外研究As the clinical candidate analog of KPT-185, KPT-330 exhibits similar effects on the viability of T-ALL cells1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEand elicits rapid apoptotic response. KPT-330 also reduces cell growth in MOLT-4, Jurkat, HBP-ALL,KO

4、PTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM 1.體內(nèi)研究 Selinexor (KPT-330) dramatically suppresses the growth of T-ALL cells (MOLT-4) and AML cells (MV411) invivo, with little toxicity to normal haematopoietic cells 1. In SCID mice with diffuse human MM bone lesions,KPT-330 inhibi

5、ts MM-induced bone lysis and prolongs survival. Moreover, KPT-330 directly impairsosteoclastogenesis and bone resorption by blocking RANKL-induced NF-B and NFATc1, with minimalimpact on osteoblasts and BMSCs 2.REFERENCES1. Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has

6、 selective anti-leukaemic activity in preclinical models ofT-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: molecularmechanisms and therapeutic implications. Leukemia. 2014 Jan;28(1):155-65.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: