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(6-(1-((6-Methoxypyridin-3-yl)methyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-yl)(4-(4-(trifluoromethyl)benzyl)piperazin-1-yl)methanone 4-?Methylbenzenesulfona?te (1:2) is an activate of Adenosine Monophosphate-Activated Protein Kinase (AMPK). Used to treat human cancer. | [in vivo]
ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression[1].
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[1].
ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min?kg)[1].
| Animal Model: | Five-week-old male nude mice with MDA-MB-453[1] | | Dosage: | 0.5, 1, 2, 4, 8 mg/kg | | Administration: | PO; once daily; for 21 days | | Result: | The tumor growth inhibition (TGI) rate was 29% at 1 mg/kg, and the tumor regression rate was 26%, 87% and 96% at 2, 4 and 8 mg/kg, respectively.
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| Animal Model: | Male SD rats[1] | | Dosage: | 1 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV or PO | | Result: | Had 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.
Had a Cmax of 72 ng/mL and an AUC24h of 705 ng?h/mL for PO.
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| [IC 50]
AMPK: 18 nM (EC50) |
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| Company Name: |
Bide Pharmatech Ltd.
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| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
| Company Name: |
InvivoChem
|
| Telephone: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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