KPT-330 |
| Catalog No.GC12467 |
KPT-330 (Selinexor) is an orally active selective inhibitor of nuclear export (SINE) compound that inhibits the nuclear export protein XPO1 (also known as CRM1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1393477-72-9
Sample solution is provided at 25 µL, 10mM.
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KPT-330 (Selinexor) is an orally active selective inhibitor of nuclear export (SINE) compound that inhibits the nuclear export protein XPO1 (also known as CRM1) [1]. KPT-330 covalently binds to the Cys528 site of XPO1, resulting in its irreversible inactivation [2]. KPT-330 can induce apoptosis, has inhibitory activity against various types of cancer cells, and can also enhance the effects of other chemotherapeutic drugs [3].
In vitro, KPT-330 (0-1000 nM) treatment of non-small cell lung cancer (NSCLC) cell lines for 72 h dose-dependently induced growth inhibition, promoted G1 phase arrest and apoptosis, and stimulated the activation of caspase-3 and caspase-9 [4]. KPT-330 (0-1000 nM) treatment of prostate cancer (PCa) cell lines for 72 h dose-dependently induced cell growth inhibition with IC50 values ranging from 43-700nM [5].
In vivo, oral treatment of mice with non-small cell lung cancer with KPT-330 (10 mg/kg) for 4 weeks significantly reduced tumor volume, reduced Ki-67-positive cells, and increased the percentage of TUNEL-positive cells, and this therapy had a synergistic effect with cisplatin [4]. Oral treatment of mice with pancreatic cancer with KPT-330 (20 mg/kg) for 3 weeks significantly reduced the expression of CRM1 protein in tumor samples, induced p27 nuclear staining, and enhanced the expression of the pro-apoptotic protein Bax [6].
References:
[1] Wang A Y, Liu H. The past, present, and future of CRM1/XPO1 inhibitors[J]. Stem cell investigation, 2019.
[2]Houghton P J, Kang M, Reynolds C P, et al. Pediatric Preclinical Testing Program (PPTP) stage 1 evaluation of the XPO1/CRM1 inhibitor KPT-330[J]. AACR (abstract LB-354), 2013.
[3]Liu S, Qiao W, Sun Q, et al. Chromosome region maintenance 1 (XPO1/CRM1) as an anticancer target and discovery of its inhibitor[J]. Journal of Medicinal Chemistry, 2021, 64(21): 15534-15548.
[4]Sun H, Hattori N, Chien W, et al. KPT-330 has antitumour activity against non-small cell lung cancer[J]. British journal of cancer, 2014, 111(2): 281-291.
[5]Gravina G L, Mancini A, Sanita P, et al. KPT-330, a potent and selective exportin-1 (XPO-1) inhibitor, shows antitumor effects modulating the expression of cyclin D1 and survivin in prostate cancer models[J]. BMC cancer, 2015, 15: 1-19.
[6]Kazim S, Malafa M P, Coppola D, et al. Selective nuclear export inhibitor KPT-330 enhances the antitumor activity of gemcitabine in human pancreatic cancer[J]. Molecular cancer therapeutics, 2015, 14(7): 1570-1581.
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