CCG-1423
目录号 : GC12795
An inhibitor of Rho-mediated cell signalling
Cas No.:285986-88-1
Sample solution is provided at 25 µL, 10mM.
CCG-1423 is a small-molecule inhibitor of RhoA transcriptional signaling. The interaction between MRTF-A and importin a/b1 was inhibited by CCG-1423, but monomeric G-actin binding to MRTF-A was not inhibited [4].
Multiple members of the Rho family of small GTPases play important roles in these cellular processes and in some human tumors (e.g., colon, esophageal, lung, pancreatic, and inflammatory breast cancers), up-regulation of RhoA or RhoC is associated with a poor clinical outcome (2, 3).
CCG-1423 has nanomolar to low micromolar potency as well as selectivity toward Rho-overexpressing and invasive cancer cell lines for inhibition of DNA synthesis, cell growth, and/or invasion. Caspase-3 activation in the highly metastatic RhoC-overexpressing A375M2 melanoma cell line was enhanced by CCG-1423 whereas a smaller increase was seen with the parental A375 cell line, whereas just the opposite pattern was seen with daunorubicin [2].
References:
[1]. Minami T, Kuwahara K, Nakagawa Y et al. Reciprocal expression of MRTF-A and myocardin is crucial for pathological vascular remodelling in mice. EMBO J. 2012 Nov 28;31(23):4428-40. doi: 10.1038/emboj.2012.296. Epub 2012 Oct 26.
[2]. Hayashi K, Watanabe B, Nakagawa Y et al. RPEL proteins are the molecular targets for CCG-1423, an inhibitor of Rho signaling. PLoS One. 2014 Feb 18;9(2):e89016. doi: 10.1371/journal.pone.0089016. eCollection 2014.
| Cas No. | 285986-88-1 | SDF | |
| 化学名 | N-((1-((4-chlorophenyl)amino)-1-oxopropan-2-yl)oxy)-3,5-bis(trifluoromethyl)benzamide | ||
| Canonical SMILES | FC(F)(F)C1=CC(C(F)(F)F)=CC(C(NOC(C)C(NC2=CC=C(Cl)C=C2)=O)=O)=C1 | ||
| 分子式 | C18H13ClF6N2O3 | 分子量 | 454.75 |
| 溶解度 | ≥ 21mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.199 mL | 10.9951 mL | 21.9901 mL |
| 5 mM | 0.4398 mL | 2.199 mL | 4.398 mL |
| 10 mM | 0.2199 mL | 1.0995 mL | 2.199 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