您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > PhiKan 083
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PhiKan 083
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。
PhiKan 083图片
CAS NO:880813-36-5
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
PhiKan 083 是一种咔唑衍生物,可与表面腔结合并稳定 Y220C(一种 p53 突变体),Kd 为 167 μM。 PhiKan 083 可用于癌症研究。
Cas No.880813-36-5
化学名1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride
Canonical SMILESCNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.Cl
分子式C16H18N2.HCl
分子量274.79
溶解度<13.74mg/ml in Water;<27.48mg/ml in DMSO
储存条件Store at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki: ≈ 150 M

PhiKan 083 is a critical p53 stabilizing agent by bonding its mutation Y220C

The mutation Y220C of p53 exists a surface cavity that destabilizes the protein by 4 kcal/mol, at a site that is not functional. A p53 stabilizing agent binding it is able to slow rate of thermal denaturation [1].

In vitro: Isothermal titration of PhiKan083 with T-p53C-Y220C exhibited 1:1 stoichiometry and a Kd of 125 ± 10 M. PhiKan083 stabilized T-p53C-Y220C in a concentration-dependent manner. In a simple binding model for PhiKan083 (T-p53C-Y220C at 310 K (37℃)), in the absence of ligand, the protein gave a half-life of 3.8 min, while it increased to 15.7 min at saturating concentrations of PhiKan083. This is a proposed anticancer drug that could be developed for the Y220C mutant using p53 stabilizing agent. The site of mutation in the oncogenic Y220C mutant PhiKan083 binds with reasonable affinity is a druggable target. Interestingly, the site of mutation does not exist in a region of the protein that is functionally important, it will be an excellent target for drug stabilization therapy. This suggests the crystal structure of the complex will be a fresh start for further rounds of drug design and refinement [1].

In vivo: So far, no study in vivo has been conducted.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Boeckler FM, Joerger AC, Jaggi G, Rutherford TJ, Veprintsev DB, Fersht AR.  Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29; 105(30):10360-5.