ASP4132

For research use only.

Catalog No.S8953

ASP4132 Chemical Structure

CAS No. 1640294-30-9

ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer.

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Biological Activity

Description ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer.
Targets
AMPK [1]
(Cell-free assay)
0.018 μM(EC50)
In vitro

ASP4132 is a new type of AMPK activator with potent AMPK activation activity and attractive selective growth inhibition against human cancer cells, improves aqueous solubility, metabolic stability and animal pharmacokinetics (PK). Studies on ASP4132 have advanced to clinical trials for the treatment of cancer.[1]

In vivo

The in vivo efficacy of ASP4132 is evaluated via MDA-MB-453 xenografts in nude mice. The tumor growth inhibition (TGI) rate is 29% at 1 mg/kg (p.o.), and the tumor regression rate is 26%, 87% and 96% at 2, 4 and 8 mg/kg, respectively. All doses of ASP4132 are well tolerated over the 21-day dosing window, and no body weight loss is observed.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: MDA-MB-453, SK-BR-3, AU565, OCUB-M,
  • Concentrations: 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 Nm
  • Incubation Time: 2 h, 4 days
  • Method:

    Each breast cancer cells above are seeded onto non-adherent 384-well white plates at 500 cells/well or 96-well white plates at 1000 cells/well. The following day, ASP4132 is added to each well at final concentrations of 0 (DMSO only), 0.3, 1, 3, 10, 30, 100, 300, 1000, and 3000 nM. The final concentration of DMSO in each well is 0.1% (v/v). Four days after addition of the test compound, cell viability was determined using a CellTiter-Glo® Luminescent Cell Viability Assay.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: five-week-old male nude mice with MDA-MB-453 xenografts
  • Dosages: 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg, 8 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (106.71 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 937.06
Formula

C46H51F3N6O8S2

CAS No. 1640294-30-9
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.COC1=NC=C(C=C1)CN2CCC(CC2)C3=CC4=C(C=C3)N=C(N4)C(=O)N5CCN(CC5)CC6=CC=C(C=C6)C(F)(F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02383368 Completed Drug: ASP4132 Lymphoma|Refractory Solid Tumors|Advanced Cancer Astellas Pharma Global Development Inc.|Astellas Pharma Inc March 23 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID