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Alflutinib (Furmonertinib) mesylate EGFR inhibitor

Name: Alflutinib (Furmonertinib) mesylate
Brand: Selleck Chemicals
SKU: S6868
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S6868

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.

Chemical Structure

Molecular Weight: 664.7

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.99

Related Targets	VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other EGFR Inhibitors	Sunvozertinib Icotinib Hydrochloride AG-490 AG-1478 Canertinib (CI-1033) Rociletinib (CO-1686) WZ4002 Genistein Poziotinib (NOV120101, HM781-36B) PD153035

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (30.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (1.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (1.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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

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	664.7	Formula	C₂₉H₃₅F₃N₈O₅S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2130958-55-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AST2818 mesylate			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

Mechanism of Action

Targets/IC₅₀/Ki	EGFR CYP3A4 (Cell-free assay) 0.25 μM(EC50)
References	[1] https://pubmed.ncbi.nlm.nih.gov/32235864/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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