产品
编 号:F750685
分子式:C25H26F3N5O3
分子量:501.5
产品类型
结构图
CAS No: 2259641-46-6
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产品详情
生物活性:
DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.
体内研究:
DS-9300 (p.o., 0.3-3 mg/kg, once daily, 33days) shows dose-dependent antitumor activity with 39%, 74% and 109% tumor growth inhibition at 0.3, 1 and 3 mg/kg, respectively, and no significant toxic effects in Castrated VCaP xenograft mouse model.The pharmacokinetic parameters of DS-9300 in BALB/c mice PO(10 mg/kg) IV(1 mg/kg) AUC, AUCu (μM*h)Cmax (μM)T1/2 (h)
体外研究:
DS-9300 inhibits the growth of prostate cancer cell lines with the IC50 values of 0.6, 6.5, 3.4 and 287.2 nM for VCaP, 22Rv1, LNCaP and PC3 cells, respectively, indicating that it could effectively inhibit the growth of prostate cancer cell lines by inhibiting histone acetylation and down-regulating PSA expression.