For research use only. Not for therapeutic Use.
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].
KPT-185 results in a significant decrease in the level of CRM1 protein and a significant accumulation of p53 in the nucleus of MV4-11 and OCI-AML3 cells[1].KPT-185 (1-1000 nM; 72 hours) dramatically reduces HPB-ALL, Jurkat, CCRF-CEM, MOLT-4, KOPTK1, LOUCY cells growth with IC50s of 16-395 nM[4].
KPT-185 leads to cell cycle arrest in G1 phase in the MOLT-4 cell line[4].
| Catalog Number | I030142 |
| CAS Number | 1333151-73-7 |
| Synonyms | propan-2-yl (Z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate |
| Molecular Formula | C16H16F3N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C16H16F3N3O3/c1-10(2)25-14(23)4-5-22-9-20-15(21-22)11-6-12(16(17,18)19)8-13(7-11)24-3/h4-10H,1-3H3/b5-4- |
| InChIKey | NLNGWFLRRRYNIL-PLNGDYQASA-N |
| SMILES | CC(C)OC(=O)C=CN1C=NC(=N1)C2=CC(=CC(=C2)OC)C(F)(F)F |
| 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. |
