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CAS No.: 1421919-75-6

KPT-276 Catalog No. CSN17829

Synonyms: KPT-276

KPT-276, analog of KPT-185, is a CRM1 blocker and acts as an orally bioavailable selective inhibitor of nuclear export (SINE) by irreversibly binding to CRM1.

规格	价格	促销价格	库存	数量

400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述KPT-276 is a selective CRM1 inhibitor which can irreversibly bind to CRM1 and block the nuclear export by mediated by CRM1. KPT-276 is an analog of KPT-185 with improved in vivo oral bioavailability and pharmacokinetics. Oral administration of 150mg/kg KPT-276, 3 times per week, for 3 weeks significantly increased the survival of the mice intravenously inoculated with human MV4-11 AML cells carrying FLT3-ITD, accompanied with significantly lower FLT3 protein expression in the spleen and lower spleen weight. KPT-276 exhibited anti-myeloma activity in vitro with IC50 values<250M for inhibition of cell viability in most HMCL cells tested post 72-hour treatment. KPT-276 led a time-dependent down-regulation of BRD4, CDC25A and c-MYC protein level in MM1.S and OCI-MY5 cells within 24h. Consistent with this, KPT-276 is synergistic in combination with JQ1 in the anti-proliferative effect on 8226, U266 and KMS18 cells. KPT-276 was capable of disrupting Ran-dependent CRM1 binding to the nuclear export sequence (NES) of the PKA inhibitor protein in vitro, a bona fide NES-containing CRM1 target. Inhibition of CRM1 through KPT-276 provide axonal protection in mouse models that are both dependent and independent of inflammation.
动物研究
剂量
Mice: 50 mg/kg, 150 mg/kg^[1] (p.o., s.c.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 50 mg/kg, 150 mg/kg^[1] (p.o., s.c.)
给药途径	p.o.

[1] Zhang K, Wang M, 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.
[2] anganathan P, Yu X, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood. 2012 Aug 30;120(9):1765-73.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3460 mL
- 11.7298 mL
- 23.4596 mL
- 5 mM
- 0.4692 mL
- 2.3460 mL
- 4.6919 mL
- 10 mM
- 0.2346 mL
- 1.1730 mL
- 2.3460 mL

技术信息

CAS号

1421919-75-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H10F8N4O

运输

蓝冰

分子量

426.26

别名

KPT-276

溶解度

DMSO	42.0 mg/mL (98.5 mM) warming
Water	insoluble

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

5 mg/mL

suspension

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