化合物PTC-028 T16680

Product Introduction
Bioactivity


英文名: PTC-028

描述: PTC-028 是一种口服有效的干细胞因子 BMI-1的抑制剂，可下调 BMI-1，诱导 caspase 介导的细胞凋亡。它选择性地抑制癌细胞，可用于治疗卵巢癌。

体外活性: PTC-028 subsequently decreases BMI-1 in the biochemical functional readout. PTC-028 (100 nM; 2-12 hours) increases the phosphorylated BMI-1 species in a time-dependent manner. uH2A is observed up to 12 h with PTC-028 (100 nM) in both CP20 and OV90 cells while total H2A levels remain unchanged. PTC-028 (100 nM; 48 hours) decreases the expression of XIAP and RIPK1 while LC3B levels remain unchanged compared to that of the control. PTC-028 (25-500 nM; 48 hours) obviously reduces CP20, OVCAR4, and OV90 epithelial ovarian cancer cell viability. However, in normal ovarian surface epithelial cells (OSE) and fallopian tube epithelial cells (FTE) cells, up to 500 nM treatment with PTC-028 for 48 hours has a minimal effect (~18-30% decrease). Significant cleavage of Caspase 7, Caspase 9, and PARP is observed in PTC-028 (100 nM; 48 hours)[1].

体内活性: PTC-028 (10 mg/kg or 20mg/kg; single oral doses) is administrated to the CD-1 mice. The Cmax is reached at both dose levels 1h post-dose after which plasma concentrations slowly decrease. PTC-028 (15 mg/kg; administered orally twice weekly) induces ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (308.40 mM)


关键字: inhibit | Inhibitor | PTC 028 | PTC-028 | PTC028 | Apoptosis

相关产品: SC-236 | Thonningianin A | Indibulin | Telomerase-IN-4 | VPC-70063 | Kaempferol | Pyrazoloacridine | Indirubin | Larotrectinib sulfate | Pranoprofen

相关库: Anti-Aging Compound Library | Cell Cycle Compound Library | Ferroptosis Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | DNA Damage & Repair Compound Library | Orally Active Compound Library | Preclinical Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途