AG-636

Catalog No.S9776 Batch:S977602

Technical Data

Formula	C₂₁H₁₇N₃O₂
Molecular Weight	343.38	CAS No.	1623416-31-8
Solubility (25°C)*	In vitro	DMSO	35 mg/mL (101.92 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.)

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Biological Activity

Description

AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.

Targets

DHODH ^[1]

In vitro

AG-636 reveals a strong enrichment in sensitivity to a novel dihydroorotate dehydrogenase (DHODH) in cancer cell lines of hematologic versus solid tumor origin.^[1]

In vivo

AG-636 results in robust tumor growth inhibition in xenograft lymphoma tumor models, with comparably poor activity in solid tumor models.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Z138 cells, OCILY19 cells, JEKO1 cells, HCT116 cells, A549 cells Concentrations 10 μM Incubation Time 96 h Method For CTG assays, cells are plated in 96-well tissue culture plates at either 10,000 cells/well for cell lines of hematologic origin or 2000 cells/well for solid tumor-derived cell lines. Cells are incubated with AG-636 or DMSO control for 96 hours. CTG readings are performed at time 0-(T0) and at time 96-hour (T96) using a Molecular Devices SpectraMAX Paradigm plate reader.
Animal Study:^{^[1]}	Animal Models Transgenic female 6-8-week-old CB17 SCID mice, Female 6-8-week-old BALB/c mice Dosages 10 mg/kg, 30 mg/kg, 100 mg/kg Administration PO

Cell Assay:^{^[1]}

Cell lines
Z138 cells, OCILY19 cells, JEKO1 cells, HCT116 cells, A549 cells
Concentrations
10 μM
Incubation Time
96 h
Method
For CTG assays, cells are plated in 96-well tissue culture plates at either 10,000 cells/well for cell lines of hematologic origin or 2000 cells/well for solid tumor-derived cell lines. Cells are incubated with AG-636 or DMSO control for 96 hours. CTG readings are performed at time 0-(T0) and at time 96-hour (T96) using a Molecular Devices SpectraMAX Paradigm plate reader.

Animal Study:^{^[1]}

Animal Models
Transgenic female 6-8-week-old CB17 SCID mice, Female 6-8-week-old BALB/c mice
Dosages
10 mg/kg, 30 mg/kg, 100 mg/kg
Administration
PO

References

[1] Gabrielle McDonald, et al. Mol Cancer Ther. 2020 Dec;19(12):2502-2515.

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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.

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