产品说明书

ASP4132

Print
Chemical Structure| 1640294-30-9 同义名 : -
CAS号 : 1640294-30-9
货号 : A1271100
分子式 : C46H51F3N6O8S2
纯度 : 97%
分子量 : 937.058
MDL号 : MFCD32693927
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(112.05 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.07mL

0.21mL

0.11mL

5.34mL

1.07mL

0.53mL

10.67mL

2.13mL

1.07mL
参考文献

[1]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