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ASP4132

Cat. No. M13362
ASP4132 Structure
Size Price Availability Quantity
5mg USD 165  USD165 In stock
10mg USD 275  USD275 In stock
25mg USD 495  USD495 In stock
50mg USD 820  USD820 In stock
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Quality Control & Documentation
Biological Activity

ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM and anticancer activity that promotes tumor regression in a xenograft mouse model of breast cancer.

Chemical Information
Molecular Weight 764.87
Formula C39H43F3N6O5S
CAS Number 1640294-30-9
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Filip Janku, et al. Invest New Drugs. First-in-human evaluation of the novel mitochondrial complex I inhibitor ASP4132 for treatment of cancer

[2] Ying-Chen Xia, et al. Cell Death Dis. AMPK activation by ASP4132 inhibits non-small cell lung cancer cell growth

[3] Kazuyuki Kuramoto, et al. Chem Pharm Bull (Tokyo). Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity

[4] Kazuyuki Kuramoto, et al. Bioorg Med Chem. 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

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Keywords: ASP4132 supplier, AMPK, inhibitors, activators


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