1443437-74-8 Usage
Uses
Used in Pharmaceutical Industry:
CCG-203971 is used as an antifibrotic agent for inhibiting fibrosis through targeting the MRTF/SRF gene transcription pathway. This makes it a potential therapeutic candidate for treating fibrosis-related conditions.
Used in Oncology:
CCG-203971 is used as an anti-proliferative agent for inhibiting the proliferation of prostate cancer cells. Its potent anti-cancer properties make it a promising candidate for the development of new treatments for prostate cancer.
Additionally, CCG-203971 may also demonstrate synergistic anti-cancer effects when combined with conventional chemotherapeutic drugs, potentially enhancing chemo-sensitivity and efficacy in resistant cases. However, this application would require further research and validation.
Biochem/physiol Actions
CCG-203971 is an inhibitor of the Rho/MKL1/SRF transcriptional pathway, which has been shown to play a role in metastasis of melanoma and breast cancer and clinically associated with castration-resistant prostate cancer. CCG-203971 is a second-generation analog of CCG-1423 (SML0987) with an IC50 of 4.2 μM vs 1 μM for CCG-1423, but less cytotoxicity. In mouse studies, CCG-203971 inhibited invasion of PC-3 prostate cancer cells and was well tolerated up to doses of 100 mg/kg IP over 5 days. The Rho/MRTF/SRF pathway has also been shown to be involved in multiple types of solid organ fibrosis. CCG-203971 repressed both matrix-stiffness and TGF-β-mediated fibrogenesis in human colonic myofibroblasts and showed antifibrotic activity in a murine model of skin injury and in pulmonary fibrosis lung fibroblasts.
Check Digit Verification of cas no
The CAS Registry Mumber 1443437-74-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,4,3,4,3 and 7 respectively; the second part has 2 digits, 7 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1443437-74:
(9*1)+(8*4)+(7*4)+(6*3)+(5*4)+(4*3)+(3*7)+(2*7)+(1*4)=158
158 % 10 = 8
So 1443437-74-8 is a valid CAS Registry Number.
1443437-74-8Relevant articles and documents
INHIBITORS OF MYOCARDIN-RELATED TRANSCRIPTION FACTOR AND SERUM RESPONSE FACTOR (MRTF/SRF)-MEDIATED GENE TRANSCRIPTION AND METHODS FOR USE OF THE SAME
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Paragraph 00138, (2016/06/01)
Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor ("MRTF/SRF"), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents
Bell, Jessica L.,Haak, Andrew J.,Wade, Susan M.,Kirchhoff, Paul D.,Neubig, Richard R.,Larsen, Scott D.
, p. 3826 - 3832 (2013/07/25)
CCG-1423 (1) is a novel inhibitor of Rho/MKL1/SRF-mediated gene transcription that inhibits invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis. We recently reported the design and synthesis of conformationally restricted analogs (e.g
