ASP4132 |
| Catalog No.GC60058 |
ASP4132 es un potente activador de AMPK activo por vÍa oral con una EC50 de 18 nM. ASP4132 tiene actividad anticancerÍgena y hace que el tumor retroceda en modelos de ratÓn con xenoinjerto de cÁncer de mama.
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Cas No.: 1640294-30-9
Sample solution is provided at 25 µL, 10mM.
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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.
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