ASP4132 is an AMPK activator with potential antineoplastic activity. Upon oral administration, ASP4132 affects oxidative phosphorylation in mitochondria of metabolically-active tumor cells, which reduces both energy production and tumor cell proliferation. Mitochondrial oxidative phosphorylation is hyperactivated in tumor cells and plays a key role in the promotion of tumor cell proliferation.
Chemical Formula: C46H51F3N6O8S2
Molecular Weight: 937.0632
Elemental Analysis: C, 58.96; H, 5.49; F, 6.08; N, 8.97; O, 13.66; S, 6.84
Chemical Name: (6-(1-((6-methoxypyridin-3-yl)methyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-yl)(4-(4-(trifluoromethyl)benzyl)piperazin-1-yl)methanone bis(4-methylbenzenesulfonate)
InChi Code: InChI=1S/C32H35F3N6O2.2C7H8O3S/c1-43-29-9-4-23(19-36-29)21-39-12-10-24(11-13-39)25-5-8-27-28(18-25)38-30(37-27)31(42)41-16-14-40(15-17-41)20-22-2-6-26(7-3-22)32(33,34)35;2*1-6-2-4-7(5-3-6)11(8,9)10/h2-9,18-19,24H,10-17,20-21H2,1H3,(H,37,38);2*2-5H,1H3,(H,8,9,10)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell.
ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM).
ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression.
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.
ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min•kg).
Kuramoto K, Yamada H, Shin T, 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;28(5):115307. doi:10.1016/j.bmc.2020.115307
Products are for research use only. Not for human use.
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