产品
编 号：F197656
分子式：C46H51F3N6O8S2
分子量：937.06
分子式：C46H51F3N6O8S2
分子量：937.06
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规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1640294-30-9
产品详情
生物活性：
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.
体内研究：
ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression. 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. ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min?kg). Animal Model:Five-week-old male nude mice with MDA-MB-453
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
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.
体外研究：
ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell. ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM).
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.
体内研究：
ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression. 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. ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min?kg). Animal Model:Five-week-old male nude mice with MDA-MB-453
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
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.
体外研究：
ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell. ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM).
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