产品
编 号:F623774
分子式:C20H18ClF6N3O2
分子量:481.82
产品类型
结构图
CAS No: 1394011-91-6
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产品详情
生物活性:
UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM.
体内研究:
UC2888 (口服灌胃;15 mg/kg;每周 3 次;4 周) 与 Imetelstat 共同处理可显著抑制肿瘤生长,并且不影响小鼠体重。 UC2288 (腹膜内注射;10 mg/kg;7 天内 4 次) 减轻 MPTP 诱导的行为障碍,防止 MPTP 处理的小鼠大脑中 MAPK 通路的激活。MPTP 处理提高了 MPTP 处理的小鼠脑中的 TNF-α、IL-6 和 IL-1β 水平,但 UC2288 显著降低 MPTP 诱导的 TNF-α、IL-6 水平,但脑中 IL-1β 没有降低。Animal Model:Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x106)
Dosage:15 mg/kg
Administration:Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
Result:Combined treatment with imetelstat synergistically inhibited tumor growth in mice.
Animal Model:MPTP-induced C57BL6 Parkinson’s disease mice model
Dosage:10 mg/kg
Administration:Intraperitoneal?injection; 4 times in 7 days
Result:Ameliorated MPTP induced PD progression through inhibition of neuroinammation.
体外研究:
UC2288 (0-10 μM;24 小时) 降低 p21 蛋白水平,但对其他蛋白没有影响。 UC2288 (0-10 μM;24 小时) 降低 p21 mRNA转录或转录后表达,但独立于 p53。