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EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM).
Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR.
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).
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