Home Protein Tyrosine Kinase EGFR inhibitor - HER2 inhibitor Epertinib hydrochloride For research use only.

Epertinib hydrochloride

Synonyms: Epertinib HCl, S-222611 hydrochloride, S-222611 HCl

Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.

Epertinib hydrochloride Chemical Structure

Epertinib hydrochloride Chemical Structure

CAS: 2071195-74-7

Purity & Quality Control

Batch: S689701 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.41%
99.41

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Biological Activity

Description Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.
Targets
EGFR [1]
(Cell-free assay)		 HER4 [1]
(Cell-free assay)		 HER2 [1]
(Cell-free assay)
1.48 nM 2.49 nM 7.15 nM

Chemical Information & Solubility

Molecular Weight 596.48 Formula

C30H28Cl2FN5O3
CAS No. 2071195-74-7 SDF --
Smiles Cl.CC#CC(=N\OCC1COCCN1)/C2=CC3=C(C=C2)N=CN=C3NC4=CC=C(OCC5=CC(=CC=C5)F)C(=C4)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (167.65 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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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