您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > CCG-100602
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：
 
CCG-100602
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。
CCG-100602图片
CAS NO:1207113-88-9
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
CCG-100602 是心肌素相关转录因子 A/血清反应因子 (MRTF-A/SRF) 信号传导的特异性抑制剂。
Cas No.1207113-88-9
化学名1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)-3-piperidinecarboxamide
Canonical SMILESClC(C=C1)=CC=C1NC(C(C2)CCCN2C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)=O
分子式C21H17ClF6N2O2
分子量478.8
溶解度≤0.2mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件4°C, protect from light
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

IC50: 9.8 μM for PC-3 prostate cancer cells

CCG-100602 is a Rho pathway inhibitor.

Rho, a member of the Ras superfamily of small GTP-binding proteins, plays a key role in various biological processes including microtubule dynamics, gene transcription, actin cytoskeleton organization, cell cycle progression, oncogenic transformation, as well as epithelial wound repair.

In vitro: CCG-100602 was developed as a CCG-1423 analog for improved selectivity, potency, and attenuated cytotoxicity. It was found that CCG-100602 was able to inhibit RhoA/C-mediated and SRF-driven luciferase expression in PC-3 prostate cancer cells. At 100 μM, CCG-100602 showed 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, having an superior efficacy-toxicity profile to that of CCG-1423 [1].

In vivo: To evaluate whether inhibition of SRF could protect podocytes from hyperglycaemia injury, daily ip administration of CCG-1423 was performed in DM rata. Results showed that CCG-1423 could ameliorate proteinuria dose-dependently. CCG-1423 at 0.02 mg/kg could significantly reduce the body weight, compared with the vehicle controls. In addition, the inhibition of SRF with CCG-1423 also significantly abrogated the reduction of synaptopodin expression and the induction of SRF,α-SMA, FSP-1 expression in renal cortex tissues [2].

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

References:
[1] Evelyn, C. R.,Bell, J.L.,Ryu, J.G., et al. Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423. Bioorganic & Medicinal Chemistry Letters 20, 665-672 (2010).
[2] Zhao L, Wang X, Sun L, Nie H, Liu X, Chen Z, Guan G.  Critical role of serum response factor in podocyte epithelial-mesenchymal transition of diabetic nephropathy. Diab Vasc Dis Res. 2016 Jan;13(1):81-92.