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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Exportin-1 (CRM1,XPO1)-KPT-276
KPT-276

Chemical Structure : KPT-276

CAS No.: 1421919-75-6

KPT-276 (KPT276)

货号: PC-49222Not For Human Use, Lab Use Only.

KPT-276 (KPT276) is an orally bioavailable selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein, shows antileukemic activity in vitro and in vivo in acute myeloid leukemia (AML).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

KPT-276 (KPT276) is an orally bioavailable selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein, shows antileukemic activity in vitro and in vivo in acute myeloid leukemia (AML).
KPT-276 inhibits a panel of AML cell lines proliferation (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1) with IC50 of 100-500 nM.
KPT-276 decreases CRM1 protein level and accumulates CRM1 cargo proteins in the nucleus.
KPT-276 induces differentiation of AML cell lines.
KPT-276 (150 mg/kg) increases survival in a human leukemia xenograft model.

物理化学性质&存储条件

分子量 426.270
分子式 C16H10F8N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

参考文献

1. Ranganathan P, et al. Blood. 2012 Aug 30;120(9):1765-73.

2. Zhang K, et al. Exp Hematol. 2013 Jan;41(1):67-78.e4.

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