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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Exportin-1 (CRM1,XPO1)-KPT-185
KPT-185

Chemical Structure : KPT-185

CAS No.: 1333151-73-7

KPT-185 (KPT185)

货号: PC-49221Not For Human Use, Lab Use Only.

KPT-185 (KPT185) is a potent, 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-185 (KPT185) is a potent, 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-185 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-185 decreases CRM1 protein level and accumulates CRM1 cargo proteins in the nucleus.
KPT-185 induces differentiation of AML cell lines.

物理化学性质&存储条件

分子量 355.317
分子式 C16H16F3N3O3
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

3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2Z-propenoic acid, 1-methylethyl ester

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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