Home Protein Tyrosine Kinase EGFR inhibitor CH7233163 For research use only.

CH7233163

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

CH7233163 Chemical Structure

CH7233163 Chemical Structure

CAS: unknown

Purity & Quality Control

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

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Biological Activity

Description CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.
Targets
EGFR [1]
In vitro
In vitro

CH7233163 shows potent antitumor activities against tumor with EGFR-Del19/T790M/C797S in vitro. CH7233163 potently inhibits the proliferation of Del19/T790M/C797S_NIH3T3 cells with IC50 of 20 nmol/L. CH7233163 potently and dose-dependently blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 can inhibit Del19/T790M/C797S signaling.[1]
Cell Research Cell lines NIH3T3 cells (ATCC)
Concentrations 8 nM, 40 nM, 200 nM, 1000 nM
Incubation Time 0.5 h-24 h, 4-7 days
Method

NIH3T3 cells (ATCC) are transduced with lentiviruses harboring genes encoding the EGFR-d746-750/T790M/C797S or EGFR-L858R/T790M/C797S mutant, generated from the pCDH-CMV-MCS-EF1-Puro vector. Cells stably expressing these mutants are subsequently selected in medium supplemented with puromycin. Cells are incubated in medium containing serial dilutions of CH7233163 in a 96-well culture plate or PrimeSurface96U plates at 37˚C for 4 or 7 d. The number of living cells is then determined using CellTiter-Glo 9 Luminescent Cell Viability Assay.
In Vivo
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. CH7233163 has potent therapeutic efficacy against tumors with EGFR-Del19/T790M/C797S in vivo.[1]
Animal Research Animal Models nude mice (CAnN.Cg-Foxn1/CrlCrlj nu/nu)
Dosages 10 mg/kg， 30 mg/kg, 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 669.72 Formula

C31H34F3N9O3S
CAS No. unknown SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (149.31 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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