MPC 6827 hydrochloride

An inhibitor of tubulin polymerization with anticancer activity

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
10mg

￥1212.00

970.00

- +
50mg

￥4825.00

3860.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci14812
CAS: 917369-31-4
别名: N-(4-甲氧基苯基)-N,2-二甲基-4-喹唑啉胺盐酸盐,MPC-6827 hydrochloride
分子式: C17H17N3O.HCl
分子量: 315.8
纯度: >98%
溶解度: ≥ 10.55mg/mL in DMSO
储存: Desiccate at RT
库存: 现货

Background

MPC-6827 (Azixa) is a small-molecule microtubule-destabilizing agent that binds to the same (or nearby) sites on β-tubulin as colchicine.[1]

Tubulin is a heterodimer consisting of an αand βmonomer, it can be covalently labeled with [3H] colchicine by near UV irradiation. Most of the label appears in β tubulin. Colchicine binds to tubulin with a stoichiometry of one and inhibits microtubule assembly substoichiometrically. Colchicine binding to tubulin exhibits pseudoirreversible kinetics; it displays a fast step followed by a slow step involving conformational changes of both ligand and tubulin. The tubulin, in turn, promotes fluorescence characteristic of the tropolone moiety of colchicine. [2]

MPC-6827 is a small-molecule microtubule-destabilizing agent that causes mitotic arrest and cell death. MPC-6827 interfere with microtubule dynamics, leading to arrest of dividing cells in the G2-M phase of the cell cycle, which eventually results in apoptotic cell death.[1]

In vivo, MPC-6827 significantly inhibits the growth of various subcutaneously implanted tumor lines. MPC-6827 has also been shown to be a vascular-disrupting agent (VDA) in a human ovarian carcinoma xenograft model. It also has shown synergism with carboplatin in a mouse xenograft model. Furthermore, MPC-6827 has been shown to inhibit the growth of human glioblastoma tumor cell line (D-54) implanted intracranially in athymic nude mice. [1]

参考文献:
[1] Tsimberidou AM1, Akerley W, Schabel MC, etal.?, Phase I clinical trial of MPC-6827 (Azixa), a microtubule destabilizing agent, in patients with advanced cancer. Mol Cancer Ther. 2010 Dec;9(12):3410-9.
[2] Uppuluri S, Knipling L, Sackett DL, Wolff J.?? Localization of the colchicine-binding site of tubulin. Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11598-602.