| Identification | Back Directory | [Name]
CCG-203971 | [CAS]
1443437-74-8 | [Synonyms]
203971
CCG-203971
CCG 203971;CCG203971;CCG-203971
N-(4-Chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide
N-(4-chlorophenyl)-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide
3-Piperidinecarboxamide, N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]- | [Molecular Formula]
C23H21ClN2O3 | [MDL Number]
MFCD28166491 | [MOL File]
1443437-74-8.mol | [Molecular Weight]
408.88 |
| Chemical Properties | Back Directory | [Boiling point ]
656.0±55.0 °C(Predicted) | [density ]
1.305±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO:81.0(Max Conc. mg/mL);198.1(Max Conc. mM) | [form ]
powder | [pka]
13.69±0.70(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
CCG 203971 acts as an antifibrotic agent, inhibiting fibrosis through targeting the MRTF/SRF gene transcription pathway. Inhibits the invasion of prostate cancer cells and acts as a potent anti-proliferative agent. | [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. | [in vivo]
CCG-203971 is tested in a Bleomycin skin injury model. Bleomycin is administered in 50 μL of DMSO intraperitoneally. Preliminary studies show that Bleomycin administered in this manner is well tolerated at 100 mg/kg twice a day. Intradermal Bleomycin for 2 weeks along with the DMSO control (50 μL i.p.) results in marked dermal thickening (P<0.0001) compared with the PBS+DMSO group, which does not receive Bleomycin. CCG-203971 treatment strongly and significantly (P<0.001) suppresses the Bleomycin-induced skin thickening in this model. Skin collagen amounts, assessed by measurement of hydroxyproline content, show similar results. Bleomycin injections promote collagen deposition (P<0.01) and CCG-203971 is able to block this effect (P<0.05)[3]. | [storage]
Store at -20°C |
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| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
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