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ASTX-029 ERK inhibitor

Cat.No.S0872

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

Batch: Purity: 99.91%
99.91

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (171.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
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%

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight 584.04 Formula

C29H31ClFN5O5

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2095719-92-7 -- Storage of Stock Solutions

Synonyms N/A SMILES COC1=CC(=CC(=C1)C(CO)NC(=O)C(C)N2CC3=CC=C(C=C3C2=O)C4=NC(=NC=C4Cl)NC5CCOCC5)F

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
ERK1
ERK2
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-02-13)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06284460 WITHDRAWN
Pathway Mutant Myelodysplastic Syndromes; Myelodysplastic Neoplasm; Myeloproliferative Neoplasm
M.D. Anderson Cancer Center
2025-01-31 PHASE1; PHASE2
NCT06113289 WITHDRAWN
Acute Myeloid Leukemia
M.D. Anderson Cancer Center
2024-02-08 PHASE1; PHASE2
NCT03520075 COMPLETED
Solid Tumor, Adult
Taiho Oncology, Inc.
2018-05-07 PHASE1; PHASE2
NCT04466514 COMPLETED
Healthy Volunteers
Astex Pharmaceuticals, Inc.
2020-07-23 PHASE1
NCT03520075 Active not recruiting
Solid Tumor Adult
Astex Pharmaceuticals Inc.
2018-05-10 Phase 1|Phase 2

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