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VU0661013
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VU0661013图片
CAS NO:2131184-57-9
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品名称
VU661013
产品介绍
VU0661013 是一种有效的选择性 MCL-1 抑制剂。

产品描述

VU0661013 is an effective and selective inhibitor of MCL-1.

体外活性

VU0661013 does not obviously suppress BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM). VU0661013 shows a Ki of 97±30 pM to human MCL-1 in a TR-FRET assay by displacing a fluorescently labeled peptide derived from the pro-apoptotic protein BAK [1].

体内活性

VU0661013 is a potent and selective MCL-1 inhibitor and is active in Venetoclax-resistant cells and patient-derived xenografts. VU0661013 treatment of disseminated human AML results in a dose-dependent decrease in tumor burden, nearly eliminating the hCD45+ MV-4-11 cells at the 75 mg/kg dose in the blood (mean, 13.0±2.2% in vehicle vs 7.4±7.2% in 25mg/kg vs 0.17±0.12% in 75 mg/kg treated mice), bone marrow (mean, 40.7±13.9% in vehicle vs 33.46±4.0 % in 25 mg/kg vs 0.384±0.345 in 75 mg/kg treated mice), and spleen (mean, 46.22±13.3% in vehicle vs 13.31±10.0% in 25 mg/kg vs 1.588±1.51% in 75 mg/kg treated mice). Treatment with VU0661013 reduces disease-associated splenomegaly (mean, vehicle vs. 75mg/kg, 0.17±0.02 vs 0.09±0.01g), and amending spleen to body weight ratio (vehicle vs 75mg/kg, 0.99 vs 0.50). In this study, NSGS mice are treated daily (starting 7 days after transplant) with vehicle only, 15 mg/kg or 75 mg/kg of VU0661013. Analysis reveals an increase in survival in mice treated with the 75mg/kg dose (vehicle treated mice=31 days, vs 15 mg/kg=32 days, vs 75 mg/kg treated mice=43 Days) [1].

Cas No.

2131184-57-9

分子式

C39H39Cl2N5O4

分子量

712.66

别名

VU661013

储存和溶解度

DMSO:117mg/mL (164.2mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years