CH7233163

Catalog No.S9711 Batch:S971101

Technical Data

Formula	C₃₁H₃₄F₃N₉O₃S
Molecular Weight	669.72	CAS No.	unknown
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (149.31 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models nude mice (CAnN.Cg-Foxn1/CrlCrlj nu/nu) Dosages 10 mg/kg， 30 mg/kg, 100 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

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

References

[1] Kenji Kashima, et al. Mol Cancer Ther. 2020 Sep 17;molcanther.0229.2020.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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