CH7233163 |
| カタログ番号GC25219 |
CH7233163は、EGFR-チロシンキナーゼの非共有結合型ATP競争阻害剤であり、EGFR-Del19/T790M/C797Sを持つ腫瘍に対する抗腫瘍活性があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: unknown
Sample solution is provided at 25 µL, 10mM.
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CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.
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]
[1] Kenji Kashima, et al. Mol Cancer Ther. 2020 Sep 17;molcanther.0229.2020.
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