CT52923

Names

[ CAS No. ]:
205256-55-9

[ Name ]:
CT52923

Biological Activity

[Description]:

CT52923 is a selective, orally active platelet-derived growth factor receptor (PDGFR) antagonist. CT52923 also is an ATP-competitive inhibitor. CT52923 can be used for the research variety of pathological diseases, including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR

[In Vitro]

CT52923 抑制 PDGFRs 和干细胞因子受体，IC50 值为 100 至 200 nM[1]。 CT52923（0.01-30 μM；24 h）阻断血小板衍生生长因子诱导的平滑肌细胞迁移或成纤维细胞增殖，IC50 分别为 64 和 280 nM[1]。 Cell Migration Assay [1] Cell Line: Rat A10 smooth muscle cells Concentration: 0.01-30 μM Incubation Time: 24 h Result: Inhibited PDGF-induced cell migration with an IC50 of 64 nM.

[In Vivo]

CT52923（口服；5、15、30 和 50 mg/kg；每日两次）可显著抑制大鼠颈动脉损伤后内膜新生的形成[1]。 Animal Model: Rat carotid artery balloon angioplasty model[1]. Dosage: 5, 15, 30, and 50 mg/kg Administration: Oral gavage; twice daily Result: Inhibited PDGF-mediated response to vascular injury.

[References]

[1]. J C Yu, et al. Efficacy of the novel selective platelet-derived growth factor receptor antagonist CT52923 on cellular proliferation, migration, and suppression of neointima following vascular injury. J Pharmacol Exp Ther. 2001 Sep;298(3):1172-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₅N₅O₄S

[ Molecular Weight ]:
467.54

Related Compounds

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