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].
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. |
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. |
[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.