MPC 6827 hydrochloride

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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。

CAS NO:

917369-31-4

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
10mg	电议
50mg	电议

产品介绍

MPC 6827 hydrochloride (MPC-6827 hydrochloride) 是一种可渗透血脑屏障的微管破坏剂，在体外和体内具有强效和广谱的细胞毒活性。 MPC 6827 hydrochloride (MPC-6827 hydrochloride) 在人 MX-1 乳腺癌和其他小鼠异种移植癌症模型中表现出有效的抗癌活性。 MPC 6827 hydrochloride (MPC 6827 hydrochloride) 是治疗多种癌症的有希望的候选药物。

Cas No.	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
化学名	N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine hydrochloride
Canonical SMILES	CN(C(C=C1)=CC=C1OC)C2=NC(C)=NC3=CC=CC=C23.Cl
分子式	C₁₇H₁₇N₃O.HCl
分子量	315.8
溶解度	≥ 10.55mg/mL in DMSO
储存条件	Desiccate at RT
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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] References: [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.