|(6-(1-((6-甲氧基吡啶-3-基)甲基)哌啶-4-基)-1H-苯并[d]咪唑-2-基)(4-(4-(三氟甲基)苄基)哌嗪-1-基)甲酮双对甲苯磺酸盐|CsnPharm

CAS No.: 1640294-30-9

ASP4132 is a new type of AMPK activator with EC50 value of 18nM. It showed attractive selective growth inhibition against human cancer cells.

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400-920-2911

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描述AMPK (adenosine monophosphate (AMP)-activated protein kinase) is a highly conserved sensor of cellular energy status, and also plays an important role in maintaining systemic energy homeostasis. ASP4132 Besylate is a potent and orally active activator of AMPK with an EC₅₀ value of 0.018 μM. ASP4132 showed cell growth inhibitory activity against MDA-MB-453 with an IC₅₀ value of 0.014 μM. In MDA-MB-453 xenografts nude mice, the tumor growth inhibition (TGI) rate was 29% at p.o. dose of 1 mg/kg, and the tumor regression rate was 26%, 87% and 96% at p.o. doses of 2, 4 and 8 mg/kg, respectively. All doses of ASP4132 were well tolerated over the 21-day dosing window^[1].
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技术信息

CAS号

1640294-30-9

储存条件

分子式

C46H51F3N6O8S2

运输

蓝冰

分子量

937.06

别名

溶解度

动物实验配方

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