1. Epigenetics PI3K/Akt/mTOR
  2. AMPK
  3. ASP4132

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.

For research use only. We do not sell to patients.

ASP4132 Chemical Structure

ASP4132 Chemical Structure

CAS No. : 1640294-30-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 256 In-stock
Solution
10 mM * 1 mL in DMSO USD 256 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 150 In-stock
10 mg USD 248 In-stock
25 mg USD 470 In-stock
50 mg USD 750 In-stock
100 mg USD 1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE ASP4132

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

AMPK

18 nM (EC50)

In Vitro

ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell[1].
ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression[1].
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[1].
ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min•kg)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old male nude mice with MDA-MB-453[1]
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[1]
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.
Clinical Trial
Molecular Weight

937.06

Formula

C46H51F3N6O8S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC2=CC=C(C3CCN(CC4=CC=C(OC)N=C4)CC3)C=C2N1)N5CCN(CC6=CC=C(C(F)(F)F)C=C6)CC5.O=S(C7=CC=C(C)C=C7)(O)=O.O=S(C8=CC=C(C)C=C8)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (106.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0672 mL 5.3358 mL 10.6717 mL
5 mM 0.2134 mL 1.0672 mL 2.1343 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.32%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0672 mL 5.3358 mL 10.6717 mL 26.6792 mL
5 mM 0.2134 mL 1.0672 mL 2.1343 mL 5.3358 mL
10 mM 0.1067 mL 0.5336 mL 1.0672 mL 2.6679 mL
15 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7786 mL
20 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3340 mL
25 mM 0.0427 mL 0.2134 mL 0.4269 mL 1.0672 mL
30 mM 0.0356 mL 0.1779 mL 0.3557 mL 0.8893 mL
40 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6670 mL
50 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5336 mL
60 mM 0.0178 mL 0.0889 mL 0.1779 mL 0.4447 mL
80 mM 0.0133 mL 0.0667 mL 0.1334 mL 0.3335 mL
100 mM 0.0107 mL 0.0534 mL 0.1067 mL 0.2668 mL
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ASP4132 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ASP4132
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