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].
ASP4132 细胞实验
Cell Line
Concentration
Treated Time
Description
References
BEAS-2B and primary lung epithelial cells
1 μM
72 h
ASP4132 had no significant effect on the viability of lung epithelial cells, showing a cancer cell-specific effect.
Cell Death Dis. 2021 Apr 6;12(4):365
A549 and NCI-H1944 cell lines
1 μM
48 h
ASP4132 significantly inhibited cell viability and proliferation, and induced apoptosis.
Cell Death Dis. 2021 Apr 6;12(4):365
Primary NSCLC cells (pNSCLC-1/-2/-3)
0.1-3.0 μM
48-72 h
ASP4132 significantly inhibited NSCLC cell growth, proliferation, cell cycle progression, migration and invasion, and induced apoptosis and programmed necrosis.
Cell Death Dis. 2021 Apr 6;12(4):365
ASP4132 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SCID mice
NSCLC xenograft model
Oral
5 mg/kg
Once daily for 21 days
Oral administration of ASP4132 significantly inhibited the growth of NSCLC xenografts without causing apparent toxicity.
搜索
