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CH5138303
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。
CH5138303图片
CAS NO:959763-06-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议

产品介绍
CH5138303 是一种有效且具有口服活性的 Hsp90 抑制剂。
Cas No.959763-06-5
别名4-[[4-氨基-6-(5-氯-1H,3H-萘并[1,8-CD]吡喃-6-基)-1,3,5-三嗪-2-基]硫基]丁酰胺
Canonical SMILESClC1=C(C2=NC(N)=NC(SCCCC(N)=O)=N2)C3=CC=CC4=C3C(COC4)=C1
分子式C19H18Cl N5O2S
分子量415.9
溶解度≥ 19.95mg/mL in DMSO
储存条件Desiccate at -20°C
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

CH5138303 is an inhibitor of Hsp90 with Kd value of 0.48 nM [1].

Heat shock protein 90 (HSP90) is a chaperone protein that stabilizes proteins against heat stress, assists proteins to fold properly and aids in protein degradation. Also, HSP90 stabilizes proteins required for tumor growth.

CH5138303 is an orally available Hsp90 inhibitor. CH5138303 showed improved water solubility with 646 μM and high affinity against Hsp90α with Kd value of 0.48 nM. In NCI-N87 cells, CH5138303 decreased the protein level and phosphorylation of Hsp90 target proteins such as Raf1, AKT, EGFR and HER2 [1].

In mice, CH5138303 exhibited high plasma clearance, oral bioavailability and total systemic exposure (AUC). In mice bearing human NCI-N87 gastric cancer xenograft model, CH5138303 exhibited potent antitumor efficacy with tumor growth inhibition (TGI) of 136% and ED50 value of 3.9 mg/kg [1].

Reference:
[1].  Suda A, Kawasaki K, Komiyama S, et al. Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors. Bioorg Med Chem, 2014, 22(2): 892-905.