Selinexor (KPT-330)是一种口服有效的选择性CRM1抑制剂,其为KPT-185的类似物。
|
英文别名 (English Synonym) |
KPT-330 |
|
中文名称 (Chinese Name) |
塞利尼索 |
|
靶点 (Target) |
CRM1 |
|
通路 (Pathway) |
Cell Cycle/DNA Damage |
|
CAS号 (CAS NO.) |
1393477-72-9 |
|
分子式 (Formula) |
C17H11F6N7O |
|
分子量 (Molecular Weight) |
443.31 |
|
纯度 (Purity) |
≥98% |
|
溶解性 (Solubility) |
溶于DMSO |
-25~-15℃保存，有效期3年
[1] Etchin J, Sanda T, Mansour MR, Kentsis A, Montero J, Le BT, Christie AL, McCauley D, Rodig SJ, Kauffman M, Shacham S, Stone R, Letai A, Kung AL, Thomas Look A. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr,161(1):117-27. doi: 10.1111/bjh.12231. Epub 2013 Feb 4. PMID: 23373539, PMCID: PMC3980736.[2]Tai YT, Landesman Y, Acharya C, Calle Y, Zhong MY, Cea M, Tannenbaum D, Cagnetta A, Reagan M, Munshi AA, Senapedis W, Saint-Martin JR, Kashyap T, Shacham S, Kauffman M, Gu Y, Wu L, Ghobrial I, Zhan F, Kung AL, Schey SA, Richardson P, Munshi NC, Anderson KC. CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications. Leukemia. 2014 Jan,28(1):155-65. doi: 10.1038/leu.2013.115. Epub 2013 Apr 16. PMID: 23588715, PMCID: PMC3883926.
