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A-1210477
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。
A-1210477图片
CAS NO:1668553-26-1
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

产品介绍
A-1210477 是一种选择性的MCL-1有效抑制剂,Ki值为 0.45 nM。它特异性结合 MCL-1,并以 MCL-1 依赖性方式促进癌细胞凋亡。

产品描述

A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki/IC50: 0.454/26.2 nM).

体外活性

In H929 cells, A-1210477 binds to MCL-1 with high affinity and induces MCL-1 protein elevation. In H929, H2110, and H23 cells, A-1210477 induce the hallmarks of apoptosis, and inhibits MCL-1-dependent cell viability. A-1210477 also synergizes with navitoclax to kill a variety of cancer cell lines. [1] In SKBR3 cells, A-1210477 inhibits MCL-1–BIM interaction and induces classical features of apoptosis. [2] In addition, A-1210477 sensitizes non-Hodgkin's lymphoma cell lines to venetoclax (ABT-199). [3]

激酶实验

Binding affinity assays: TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52?mM monobasic potassium phosphate, 15.48?mM dibasic potassium phosphate, 1?mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50?mM sodium chloride, and 1?mM DTT (pH 7.5). For MCL-1 assays, GST-tagged MCL-1 (1?nM) is mixed with 100?nM f-Bak, 1?nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60?min. Fluorescence is measured on an Envision plate reader using a 340/35?nm excitation filter and 520/525 (f-Bak) and 495/510?nm (Tb-labeled anti-GST antibody) emission filters.

细胞实验

Adherent cell lines are seeded at 50?000 cells per well in 96-well plates and treated for 48?h with compounds diluted in half-log steps starting at 30?μM and ending at 0.001?μM. Multiple myeloma cell lines were seeded at 15?000–20?000 cells per well and treated similarly. Effects on proliferation and viability were determined using CellTiter-Glo reagent according to the manufacturer's instructions. IC50 values are determined by non-linear regression analysis of the concentration response data.(Only for Reference)

Cas No.

1668553-26-1

分子式

C46H55N7O7S

分子量

850.05

储存和溶解度

DMSO:Insoluble
H2O:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years