ASP4132

Catalog No.S8953 Batch:S895301

Technical Data

Formula	C₄₆H₅₁F₃N₆O₈S₂
Molecular Weight	937.06	CAS No.	1640294-30-9
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (106.71 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	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

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

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

References

[1] Kazuyuki Kuramoto, et al. Bioorg Med Chem. 2020 Mar 1;28(5):115307.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.