Art. -Nr.: HY-136447

ASP4132

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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.

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Reinheit: 99.81%
CAS. Nr.: 1640294-30-9
Formel: C₄₆H₅₁F₃N₆O₈S₂
Molecular Weight:937.06

Speicherung:

4°C, sealed storage, away from moisture

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

ASP4132 Chemical Structure

CAS. Nr.: 1640294-30-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle AMPK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-435	EC₅₀	0.018 μM Compound: 28; ASP4132	Activation of AMPK in human MDA-MB-435 cells measured after 2 hrs by anti-phospho-Acetyl-CoA Carboxylase (Ser79) antibody-based ELISA Activation of AMPK in human MDA-MB-435 cells measured after 2 hrs by anti-phospho-Acetyl-CoA Carboxylase (Ser79) antibody-based ELISA	[PMID: 32007387]
MDA-MB-453	IC₅₀	0.014 μM Compound: 28; ASP4132	Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay	[PMID: 32007387]
SK-BR-3	IC₅₀	>3 μM Compound: 28; ASP4132	Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay	[PMID: 32007387]

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 T_1/2 of 3.6 hours, a CL_tot of 19 mL/min?kg, and a V_ss of 4.6 L/kg for rats for IV^[1].
ASP4132 is stable in human liver microsomes (HLM CL_{int, 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 T_1/2 of 3.6 hours, a CL_tot of 19 mL/min•kg, and a V_ss of 4.6 L/kg for rats for IV.
Had a C_max of 72 ng/mL and an AUC_24h of 705 ng∙h/mL for PO.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1640294-30-9
Appearance Solid
Molecular Weight 937.06
Formel C₄₆H₅₁F₃N₆O₈S₂
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (1)

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Journal Impact Factor

Cell Death Dis

AMPK activation by ASP4132 inhibits non-small cell lung cancer cell growth. [Abstract]

2021 Apr 6;12(4):365. PMID: 33824293

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0672 mL

5.3358 mL

10.6717 mL

5 mM

0.2134 mL

1.0672 mL

2.1343 mL

10 mM

0.1067 mL

0.5336 mL

1.0672 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kazuyuki Kuramoto, et al. Development of a Potent and Orally Active Activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK), ASP4132, as a Clinical Candidate for the Treatment of Human Cancer. Bioorg Med Chem. 2020 Mar 1;28(5):115307. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

ASP4132

1 Cited Publications

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ASP4132

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High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ASP4132

Alle AMPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ASP4132

Epigenetics Compound Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Activators Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ASP4132

Alle AMPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ASP4132 Related Classifications

HY-136447 Related Classifications