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ASP4132
CAS No. 1640294-30-9
ASP4132( —— )
Catalog No. M22042 CAS No. 1640294-30-9
ASP4132 is an orally active AMPK activator (EC50 : 18 nM), has anti-cancer activity.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 195 | In Stock |
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| 5MG | 117 | In Stock |
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| 10MG | 187 | In Stock |
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| 25MG | 339 | In Stock |
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| 50MG | 498 | In Stock |
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| 100MG | 700 | In Stock |
|
| 200MG | 958 | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameASP4132
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NoteResearch use only, not for human use.
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Brief DescriptionASP4132 is an orally active AMPK activator (EC50 : 18 nM), has anti-cancer activity.
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DescriptionASP4132 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).
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In VitroASP4132 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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In VivoASP4132 (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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Synonyms——
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PathwayMembrane Transporter/Ion Channel
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TargetAMPK
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RecptorAMPK
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Research Area——
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Indication——
Chemical Information
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CAS Number1640294-30-9
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Formula Weight937.06
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Molecular FormulaC46H51F3N6O8S2
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Purity>98% (HPLC)
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SolubilityDMSO:230 mg/mL (245.45 mM; Need ultrasonic); Methanol:8.33 mg/mL (8.89 mM; Need ultrasonic)
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SMILESCC1=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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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Kazuyuki Kuramoto , Yuki Sawada, Tomohiro Yamada,et al.Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity.Chem Pharm Bull (Tokyo). 2020;68(5):452-465.
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