CCG-100602
目录号 : GC14986
A Rho/MKL1 transcriptional pathway inhibitor
Cas No.:1207113-88-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1207113-88-9 | SDF | |
| 化学名 | 1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)-3-piperidinecarboxamide | ||
| Canonical SMILES | ClC(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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0886 mL | 10.4428 mL | 20.8855 mL |
| 5 mM | 0.4177 mL | 2.0886 mL | 4.1771 mL |
| 10 mM | 0.2089 mL | 1.0443 mL | 2.0886 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet