ASP4132 是一种具有口服活性，有效的 AMPK 激活剂，EC50 为 18 nM。ASP4132 具有抗癌活性，可在乳腺癌异种移植小鼠模型中促使肿瘤消退。
货号:ajcx29132
CAS:1640294-30-9
分子式:C46H51F3N6O8S2
分子量：937.06
溶解度:DMSO: 250 mg/mL (266.79 mM); Methanol: 8.33 mg/mL (8.89 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models[1].

ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell[1]. ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM)[1].

ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression[1]. ASP4132 (1 mg/kg; IV or PO) has a T1/2 of 3.6 hours, a CLtot of 19 mL/min•kg, and a Vss of 4.6 L/kg for rats for IV[1]. ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min/kg)[1]. Animal Model: Five-week-old male nude mice with MDA-MB-453[1]

[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.