1640294-30-9
1640294-30-9 structure
- Name: ASP4132
- Chemical Name: ASP4132
- CAS Number: 1640294-30-9
- Molecular Formula: C46H51F3N6O8S2
- Molecular Weight: 937.06
- Catalog: Signaling Pathways Epigenetics AMPK
- Create Date: 2020-08-08 17:28:33
- Modify Date: 2024-01-10 09:16:15
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ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models[1].
| Name | ASP4132 |
|---|
| Description | ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models[1]. |
|---|---|
| Related Catalog | |
| Target |
AMPK:18 nM (EC50) |
| In Vitro | ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell[1]. ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM)[1]. |
| 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. 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. |
| References |
| Molecular Formula | C46H51F3N6O8S2 |
|---|---|
| Molecular Weight | 937.06 |