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PhiKan 083 Sale

目录号 : GC12658

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。

PhiKan 083 Chemical Structure

Cas No.:880813-36-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,180.00
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1mg
¥450.00
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5mg
¥990.00
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10mg
¥1,584.00
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25mg
¥2,880.00
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50mg
¥4,320.00
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Sample solution is provided at 25 µL, 10mM.

Description

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°C)), 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.

化学性质

Cas No. 880813-36-5 SDF
化学名 1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride
Canonical SMILES CNCC1=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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.6391 mL 18.1957 mL 36.3914 mL
5 mM 0.7278 mL 3.6391 mL 7.2783 mL
10 mM 0.3639 mL 1.8196 mL 3.6391 mL
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