Bioactivity | PKT-276, an analogue of PKT-185, is an oral bioavailable and selective inhibitor of nuclear output (SINE). PKT-276 is also a CRM1 antagonist that irreversibly binds to and blocks the function of CRM1[1]. | ||||||||||||
Name | KPT-276 | ||||||||||||
CAS | 1421919-75-6 | ||||||||||||
Formula | C16H10F8N4O | ||||||||||||
Molar Mass | 426.26 | ||||||||||||
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]. 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. [3]. Schmidt J, et al. Genome-wide studies in multiple myeloma identify XPO1/CRM1 as a critical target validated using the selective nuclear export inhibitor KPT-276. Leukemia. 2013 Dec;27(12):2357-65. |