| Bioactivity | KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity[1][2]. |
| Invitro | KPT-251 binds in the NES-binding groove, which is located on the central, convex side of the CRM1 ring[1].KPT-251 (72 h) suppresses melanoma cell proliferation[2].KPT-251 (1 μM; 0-48 h) modulates levels of p53, pRb, survivin, and ERK phosphorylation[2].KPT-251 (0.1 and 1 μM; 0-72 h) induces cell-cycle arrest and apoptosis[2]. Western Blot Analysis[2] Cell Line: |
| In Vivo | KPT-251 (75 mg/kg/day; i.g.; three times per week for 5 weeks) effectively suppresses the growth of MV4-11 cells engrafted into NSG mice and provides a significant survival benefit[1].KPT-251 (50 mg/kg; p.o.; every other day for 21 days) suppresses tumor growth in mice melanoma xenograft models[2]. Animal Model: |
| Name | KPT-251 |
| CAS | 1388841-50-6 |
| Formula | C14H7F6N5O |
| Molar Mass | 375.23 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Etchin J, et al. Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells. Leukemia. 2013 Jan;27(1):66-74. [2]. 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. |