Home MAPK ERK inhibitor ASTX-029 For research use only.

ASTX-029

ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival.

ASTX-029 Chemical Structure

ASTX-029 Chemical Structure

CAS No. 2095719-92-7

Purity & Quality Control

ASTX-029 Related Products

Signaling Pathway

ERK Signaling Pathways

ERK Signaling Pathway

Biological Activity

Description ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival.
Targets
ERK1 [1] ERK2 [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03520075 Active not recruiting
Solid Tumor Adult
Astex Pharmaceuticals Inc.
 May 10 2018 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 584.04 Formula

C29H31ClFN5O5
CAS No. 2095719-92-7 SDF --
Smiles COC1=CC(=CC(=C1)C(CO)NC(=O)C(C)N2CC3=CC=C(C=C3C2=O)C4=NC(=NC=C4Cl)NC5CCOCC5)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (171.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : 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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