化合物 EGFR/HER2/DHFR-IN-1 T61596
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | 价格 | 操作 |
---|---|---|
25 mg | ¥10,600.00 | 询底价 |
100 mg | ¥17,500.00 | 询底价 |
50 mg | ¥13,800.00 | 询底价 |
Product Introduction
Bioactivity
英文名: EGFR/HER2/DHFR-IN-1
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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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