Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 348 | 现货 | ||
2 mg | ¥ 493 | 现货 | ||
5 mg | ¥ 772 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,530 | 现货 | ||
50 mg | ¥ 3,790 | 现货 | ||
100 mg | ¥ 5,450 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 866 | 现货 |
产品描述 | PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis. |
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]. |
分子量 | 405.32 |
分子式 | C19H12F5N5 |
CAS No. | 1782970-28-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (308.40 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4672 mL | 12.3359 mL | 24.6719 mL | 61.6797 mL |
5 mM | 0.4934 mL | 2.4672 mL | 4.9344 mL | 12.3359 mL | |
10 mM | 0.2467 mL | 1.2336 mL | 2.4672 mL | 6.168 mL | |
20 mM | 0.1234 mL | 0.6168 mL | 1.2336 mL | 3.084 mL | |
50 mM | 0.0493 mL | 0.2467 mL | 0.4934 mL | 1.2336 mL | |
100 mM | 0.0247 mL | 0.1234 mL | 0.2467 mL | 0.6168 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PTC-028 1782970-28-8 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair BMI-1 inhibit Inhibitor PTC 028 PTC028 inhibitor