| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87669-5mg |
98% | ￥1210.00 |
10 | - | - | - | - |
|
S87669-25mg |
98% | ￥3990.00 |
8 | - | - | - | - |
|
| 产品描述： | ASP4132 是一种 Adenosine Monophosphate-Activated Protein Kinase (AMPK) 的有效口服活性激活剂，其对应的EC50值为0.018 μM。ASP4132 可用作治疗人类癌症的临床候选药物 | ||||||||||||||||||||
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| 靶点： | AMPK(Cell-free assay):0.018 μM(EC50);AMPK | ||||||||||||||||||||
| 体外研究： | ASP4132 is a new type of AMPK activator with potent AMPK activation activity and attractive selective growth inhibition against human cancer cells, improves aqueous solubility, metabolic stability and animal pharmacokinetics (PK). Studies on ASP4132 have advanced to clinical trials for the treatment of cancer | ||||||||||||||||||||
| 体内研究： | The in vivo efficacy of ASP4132 is evaluated via MDA-MB-453 xenografts in nude mice. The tumor growth inhibition (TGI) rate is 29% at 1 mg/kg (p.o.), and the tumor regression rate is 26%, 87% and 96% at 2, 4 and 8 mg/kg, respectively. All doses of ASP4132 are well tolerated over the 21-day dosing window, and no body weight loss is observed | ||||||||||||||||||||
| 细胞实验： | Cell lines: MDA-MB-453, SK-BR-3, AU565, OCUB-M, Concentrations: 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 Nm Incubation Time: 2 h, 4 days Method: Each breast cancer cells above are seeded onto non-adherent 384-well white plates at 500 cells/well or 96-well white plates at 1000 cells/well. The following day, ASP4132 is added to each well at final concentrations of 0 (DMSO only), 0.3, 1, 3, 10, 30, 100, 300, 1000, and 3000 nM. The final concentration of DMSO in each well is 0.1% (v/v). Four days after addition of the test compound, cell viability was determined using a CellTiter-Glo® Luminescent Cell Viability Assay. | ||||||||||||||||||||
| 动物实验： | Animal Models: five-week-old male nude mice with MDA-MB-453 xenografts Dosages: 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg, 8 mg/kg Administration: Oral gavage | ||||||||||||||||||||
| 参考文献： | 1. Kazuyuki Kuramoto, et al. Development of a potent and orally active activator of adenosine monophosphate-activated protein kinase (AMPK), ASP4132, as a clinical candidate for the treatment of human cancer. Bioorg Med Chem. 2020 Mar 1;28(5):115307. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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北京