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KPT-276 is a selective inhibitor of nuclear transport (SINE) that targets the export protein CRM1 (also known as XPO1). KPT-276 was shown to suppress tumor growth without major toxic effects in mice with Jeko-1 xenograft. In vivo treatment of human multiple myeloma cell lines was shown to reduce viability of the cells, to reduce levels of c-Myc, CDC25A, and BRD4, and to induce cell cycle arrest.
| Cas No. | 1421919-75-6 |
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| Purity | ≥99% |
| Formula | C16H10F8N4O |
| Formula Wt. | 426.27 |
| Chemical Name | (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one |
| IUPAC Name | (2Z)-3-{3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}-1-(3,3-difluoro-1-azetidinyl)-2-propen-1-one |
| Synonym | KPT276 |
| Solubility | DMSO, 20 mg/mL (46.9 mM). Water, Insoluble. Ethanol, Insoluble |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Han X, Wang J, Shen Y, et al. CRM1 as a new therapeutic target for non-Hodgkin lymphoma. Leuk Res. 2015 Jan;39(1):38-46. PMID: 25466285.
Green AL, Ramkissoon SH, McCauley D, et al. Preclinical antitumor efficacy of selective exportin 1 inhibitors in glioblastoma. Neuro Oncol. 2015 May; 17(5):697-707. PMID: 25366336.
Schmidt J, Braggio E, Kortuem KM, 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):2357-2365. PMID: 23752175.