CH7233163 是一种EGFR-tyrosine kinase 的非共价ATP 竞争性抑制剂，对有EGFR-Del19/T790M/C797S 的肿瘤具有抗肿瘤活性。

EGFR:

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]

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]

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.