Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 10-14周 | ||
50 mg | ¥ 13,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
产品描述 | EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1]. |
体外活性 | EGFR/HER2-IN-7 (compound 39) shows remarkable broad spectrum cytotoxic potency, with an IC 50 value of 1.83 μM against MCF-7 breast cancer cell lines [1]. EGFR/HER2-IN-7 (1.83 μM) induces cell apoptosis by arreating cell cycle at G1/S [1]. Cell Cycle Analysis [1] Cell Line: HepG2 hepatocellular carcinoma, MCF-7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate and Hea cervical epithelioid carcinoma Concentration: 0-1 mM Incubation Time: 72 hours Result: Inhibited EGFR/HER2 kinase and DHFR, while DHFR inhibition caused cell cycle arrest at the S phase while EGFR/HER2 kinase inhibition caused arrest at the G1 phase. Apoptosis Analysis [1] Cell Line: HepG2 hepatocellular carcinoma, MCF-7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate and Hea cervical epithelioid carcinoma Concentration: 0-1 mM Incubation Time: 72 hours Result: Inhibited cancer cells growth and induced apopsosis with IC 50 s of 3.48 μM (HepG2), 1.83 μM (MCF-7), 6.08 μM (HCT-116), 12.74 μM (PC3), 4.78 μM (Hela), respectively. |
体内活性 | Caspase-3 is a lysosomal enzyme involved in apoptosis, and is used as a biomarker for detection of apoptotic cells [1]. EGFR/HER2-IN-7 (compound 39) (10 mg/kg; i.p.; once daily; 20 d) shows anti-breast cancer activity in vivo and increases caspase-3 immunoexpression in brease cancer mice [1]. Animal Model: Breast cancer with non-lactating mammary glands animal model in Swiss albino female mice (8-weeks-old) [1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; once daily; 20 days Result: Inhibited tumor volume with reduction rate of 76.5%. Reduced body weight with loss rate of 17.4%. Showed the Caspase-3 score of 1.33. |
分子量 | 379.23 |
分子式 | C14H11BrN4O2S |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
EGFR/HER2/DHFR-IN-1 Inhibitor inhibitor inhibit