ASP4132

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ASP4132 是一种口服活性 AMPK 激活剂 (EC50 : 18 nM)，具有抗癌活性。

ASP4132 is an orally active AMPK activator (EC50 : 18 nM), has anti-cancer activity.(In Vitro):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).(In Vivo):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).

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 (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.

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Membrane Transporter/Ion Channel

AMPK

AMPK

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1640294-30-9

937.06

C46H51F3N6O8S2

>98% (HPLC)

DMSO:230 mg/mL (245.45 mM; Need ultrasonic); Methanol:8.33 mg/mL (8.89 mM; Need ultrasonic)

CC1=CC=C(C=C1)S(O)(=O)=O.CC1=CC=C(C=C1)S(O)(=O)=O.COC1=CC=C(CN2CCC(CC2)C2=CC=C3N=C(NC3=C2)C(=O)N2CCN(CC3=CC=C(C=C3)C(F)(F)F)CC2)C=N1

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(-20℃)

With Ice Pack

≥ 2 years