Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 298 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,890 | 现货 | ||
50 mg | ¥ 4,360 | 现货 | ||
100 mg | ¥ 6,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 788 | 现货 |
产品描述 | TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR. |
体外活性 | TD52 dihydrochloride (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines. TD52 dihydrochloride (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression. TD52 dihydrochloride (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt. TD52 dihydrochloride (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells. TD52 dihydrochloride (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2[1]. |
体内活性 | TD52 dihydrochloride (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight[1]. |
别名 | TD52 dihydrochloride(1798328-24-1 Free base), TD52 2HCl |
分子量 | 433.33 |
分子式 | C24H18Cl2N4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (51.9 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3077 mL | 11.5386 mL | 23.0771 mL | 57.6928 mL |
5 mM | 0.4615 mL | 2.3077 mL | 4.6154 mL | 11.5386 mL | |
10 mM | 0.2308 mL | 1.1539 mL | 2.3077 mL | 5.7693 mL | |
20 mM | 0.1154 mL | 0.5769 mL | 1.1539 mL | 2.8846 mL | |
50 mM | 0.0462 mL | 0.2308 mL | 0.4615 mL | 1.1539 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。
TD52 dihydrochloride Others TD52 dihydrochloride(1798328-24-1 Free base) TD 52 Dihydrochloride TD52 TD-52 TD52 Dihydrochloride TD52 2HCl TD 52 TD-52 Dihydrochloride Inhibitor inhibitor inhibit