Alflutinib (AST2818) mesylate

Catalog No.S6868 Synonyms: Furmonertinib mesylate

For research use only.

Alflutinib (AST2818, Furmonertinib) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.

Alflutinib (AST2818) mesylate Chemical Structure

CAS No. 2130958-55-1

Purity & Quality Control

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Biological Activity

Description Alflutinib (AST2818, Furmonertinib) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.
Targets
EGFR [1]
()
CYP3A4 [1]
(Cell-free assay)
0.25 μM(EC50)

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 20 mg/mL
(30.08 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 664.7
Formula

C29H35F3N8O5S

CAS No. 2130958-55-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(N=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OCC(F)(F)F

In vivo Formulation Calculator (Clear solution)

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

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%DMSO %

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03941340 Completed Drug: [14]-AST2818 Healthy Male Volunteers Allist Pharmaceuticals Inc. April 8 2019 Phase 1
NCT03926182 Completed Drug: AST2818 Tablets Healthy Male Volunteers Allist Pharmaceuticals Inc. February 19 2019 Phase 1
NCT03452592 Unknown status Drug: Alflutinib Advanced NSCLC Patients With T790M Allist Pharmaceuticals Inc. April 30 2018 Phase 2
NCT03127449 Unknown status Drug: Alflutinib Advanced NSCLC Allist Pharmaceuticals Inc. June 1 2017 Not Applicable
NCT02973763 Unknown status Drug: Alflutinib NSCLC Allist Pharmaceuticals Inc. December 30 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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