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CCG-203971

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Chemical Structure| 1443437-74-8 同义名 : -
CAS号 : 1443437-74-8
货号 : A415352
分子式 : C23H21ClN2O3
纯度 : 99%+
分子量 : 408.88
MDL号 : MFCD28166491
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(611.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Rho-subclass
描述 CCG-203971, a novel inhibitor of Rho-mediated gene transcription. CCG-203971 is efficacious in multiple animal models of acute fibrosis, including scleroderma, when given intraperitoneally[3]. CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM[4]. CCG-203971 has a significant reduction of melanoma metastasis and bleomycin- induced fibrosis[5]. CCG-203971, is also a novel small-molecule inhibitor of MRTF/SRF-regulated transcription, inhibits expression of connective tissue growth factor (CTGF), α-smooth muscle actin (α-SMA), and collagen 1 (COL1A2) in both SSc fibroblasts and in lysophosphatidic acid (LPA)-and transforming growth factor β (TGFβ)-stimulated fibroblasts. In vivo treatment with CCG-203971 also prevented bleomycin-induced skin thickening and collagen deposition[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.24mL

12.23mL

2.45mL

1.22mL

24.46mL

4.89mL

2.45mL
参考文献

[1]Johnson LA, Rodansky ES, et al. Optimisation of Intestinal Fibrosis and Survival in the Mouse S. Typhimurium Model for Anti-fibrotic Drug Discovery and Preclinical Applications. J Crohns Colitis. 2016 Dec 16. pii: jjw210.

[2]Haak AJ, Appleton KM, et al. Pharmacological Inhibition of Myocardin-related Transcription Factor Pathway Blocks Lung Metastases of RhoC-Overexpressing Melanoma. Mol Cancer Ther. 2017 Jan;16(1):193-204.

[3]Hutchings KM, Lisabeth EM, Rajeswaran W, Wilson MW, Sorenson RJ, Campbell PL, Ruth JH, Amin A, Tsou PS, Leipprandt JR, Olson SR, Wen B, Zhao T, Sun D, Khanna D, Fox DA, Neubig RR, Larsen SD. Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1744-1749

[4]Bell JL, Haak AJ, Wade SM, Kirchhoff PD, Neubig RR, Larsen SD. Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3826-32

[5]Lisabeth EM, Kahl D, Gopallawa I, Haynes SE, Misek SA, Campbell PL, Dexheimer TS, Khanna D, Fox DA, Jin X, Martin BR, Larsen SD, Neubig RR. Identification of Pirin as a Molecular Target of the CCG-1423/CCG-203971 Series of Antifibrotic and Antimetastatic Compounds. ACS Pharmacol Transl Sci. 2019 Apr 12;2(2):92-100

[6]Haak AJ, Tsou PS, Amin MA, Ruth JH, Campbell P, Fox DA, Khanna D, Larsen SD, Neubig RR. Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury. J Pharmacol Exp Ther. 2014 Jun;349(3):480-6