Home Protein Tyrosine Kinase EGFR inhibitor CH7233163

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CH7233163 EGFR inhibitor

Cat.No.S9711

CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.
CH7233163 EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 669.72

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Quality Control

Batch: S971101 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.91%
98.91

Chemical Information, Storage & Stability

Molecular Weight 669.72 Formula

C31H34F3N9O3S

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (149.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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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Mechanism of Action

Targets/IC50/Ki
EGFR [1]
In vitro

CH7233163 shows potent antitumor activities against tumor with EGFR-Del19/T790M/C797S in vitro. This compound potently inhibits the proliferation of Del19/T790M/C797S_NIH3T3 cells with IC50 of 20 nmol/L. It potently and dose-dependently blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. This chemical can inhibit Del19/T790M/C797S signaling.[1]
In vivo

Pharmacodynamic study is performed using Del19/T790M/C797S_NIH3T3 xenografted tumors in mice. CH7233163 clearly inhibits EGFR phosphorylation after oral administration and potent tumor regression is observed. This compound has potent therapeutic efficacy against tumors with EGFR-Del19/T790M/C797S in vivo.[1]
References

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