AG-636

Catalog No.S9776

For research use only.

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

AG-636 Chemical Structure

CAS No. 1623416-31-8

Purity & Quality Control

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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 Research:

[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 Research:

[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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 343.38
Formula

C21H17N3O2

CAS No. 1623416-31-8
Storage 3 years -20°C powder
2 years -80°C in solvent

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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