CH7233163

For research use only.

Catalog No.S9711

CH7233163 Chemical Structure

CAS No. unknown

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

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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

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]

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: nude mice (CAnN.Cg-Foxn1/CrlCrlj nu/nu)
  • Dosages: 10 mg/kg, 30 mg/kg, 100 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (149.31 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 669.72
Formula

C31H34F3N9O3S

CAS No. unknown
Storage powder
in solvent
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID