Home Metabolism Dehydrogenase inhibitor AG-636 For research use only.

AG-636

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

AG-636 Chemical Structure

AG-636 Chemical Structure

CAS: 1623416-31-8

Purity & Quality Control

Batch: Purity: 99.89%
99.89

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Signaling Pathway

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Dehydrogenase Signaling Pathway

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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
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]
Cell Research 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.
In Vivo
In vivo

AG-636 results in robust tumor growth inhibition in xenograft lymphoma tumor models, with comparably poor activity in solid tumor models.[1]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03834584 Terminated
Lymphoma
Agios Pharmaceuticals Inc.
 May 24 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 343.38 Formula

C21H17N3O2
CAS No. 1623416-31-8 SDF --
Smiles C[N]1N=NC2=CC(=CC(=C12)C(O)=O)C3=CC=C(C=C3)C4=CC=CC=C4C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 35 mg/mL ( (101.92 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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