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ASP4132 AMPK activator

Name: ASP4132
Brand: Selleck Chemicals
SKU: S8953
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8953

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

Chemical Structure

Molecular Weight: 937.06

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Quality Control

Batch: S895301 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.09%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.09

Related Targets	PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK
Other AMPK Inhibitors	Dorsomorphin Dihydrochloride Dorsomorphin (Compound C) AICAR (Acadesine) A-769662 GSK621 WZ4003 ex229 (compound 991) Phenformin HCl BAY-3827 HTH-01-015

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (106.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (5.34mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.4mg/ml (0.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	937.06	Formula	C₄₆H₅₁F₃N₆O₈S₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1640294-30-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Mechanism of Action

Targets/IC₅₀/Ki	AMPK (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 this compound have advanced to clinical trials for the treatment of cancer.
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 this compound are well tolerated over the 21-day dosing window, and no body weight loss is observed.
References	[1] https://pubmed.ncbi.nlm.nih.gov/32007387/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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