| Bioactivity | KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts[1]. | ||||||||||||
| Target | CRM1 | ||||||||||||
| Invitro | KPT-185 导致 MV4-11 和 OCI-AML3 细胞细胞核中 CRM1 蛋白水平显著降低，p53 显著积累[1]。KPT-185 (1-1000 nM；72 h) 显著降低 HPB-ALL、Jurkat、CCRF-CEM、MOLT-4、KOPTK1、LOUCY 细胞的生长，IC50 为 16-395 nM[4]。KPT-185 导致 MOLT-4 细胞系在 G1 期细胞周期阻滞[4]。 Cell Viability Assay[4] Cell Line: | ||||||||||||
| Name | KPT-185 | ||||||||||||
| CAS | 1333151-73-7 | ||||||||||||
| Formula | C16H16F3N3O3 | ||||||||||||
| Molar Mass | 355.31 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ranganathan P, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood. 2012 Aug 30;120(9):1765-73. [2]. Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activityin preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr;161(1):117-27. [3]. Zhang K, et al. Novel selective inhibitors of nuclear export CRM1 antagonists for therapy in mantle cell lymphoma. Exp Hematol. 2013 Jan;41(1):67-78.e4. [4]. Salas Fragomeni RA, et al. CRM1 and BRAF inhibition synergize and induce tumor regression in BRAF-mutant melanoma. Mol Cancer Ther. 2013 Jul;12(7):1171-9. |
KPT-185
CAS: 1333151-73-7 F: C16H16F3N3O3 W: 355.31
KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at su
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