Home Protein Tyrosine Kinase EGFR inhibitor - P450 (e.g. CYP17) activator Alflutinib (Furmonertinib) mesylate For research use only.

Alflutinib (Furmonertinib) mesylate

Synonyms: AST2818 mesylate

Alflutinib (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 (Furmonertinib) mesylate Chemical Structure

Alflutinib (Furmonertinib) mesylate Chemical Structure

CAS: 2130958-55-1

Selleck's Alflutinib (Furmonertinib) mesylate has been cited by 1 publication

Purity & Quality Control

Batch: S686801 DMSO] 20 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.99%
99.99

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Biological Activity

Description Alflutinib (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)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05364073 Recruiting Non-Small Cell Lung Cancer (NSCLC)|Metastatic Non-Small Cell Lung Cancer|Advanced Non-Small Cell Lung Cancer|HER2 Exon 20 Mutations|EGFR Exon 20 Mutations|EGFR Uncommon Mutations Including G719X and S768I ArriVent BioPharma Inc. June 30 2022 Phase 1
NCT03941340 Completed Healthy Male Volunteers Allist Pharmaceuticals Inc. April 8 2019 Phase 1
NCT03926182 Completed Healthy Male Volunteers Allist Pharmaceuticals Inc. February 19 2019 Phase 1
NCT03452592 Unknown status Advanced NSCLC Patients With T790M Allist Pharmaceuticals Inc. April 30 2018 Phase 2
NCT03127449 Unknown status Advanced NSCLC Allist Pharmaceuticals Inc. June 1 2017 Not Applicable

Chemical lnformation & Solubility

Molecular Weight 664.7 Formula

C29H35F3N8O5S
CAS No. 2130958-55-1 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 20 mg/mL ( (30.08 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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.

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