AG-636

For research use only.

Catalog No.S9776

AG-636 Chemical Structure

CAS No. 1623416-31-8

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

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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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL (101.92 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 343.38
Formula

C21H17N3O2

CAS No. 1623416-31-8
Storage powder
in solvent
Synonyms N/A

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03834584 Terminated Drug: AG-636 Lymphoma Agios Pharmaceuticals Inc. May 24 2019 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID