DA-0157 is a selective inhibitor of the epidermal growth factor receptor (EGFR) and anaplastic lymphoma kinase (ALK), designed to address drug-resistant mutations, specifically EGFR C797S and ALK mutations in non-small cell lung cancer (NSCLC) models. It demonstrates potent antiproliferative activity in cells bearing EGFR Del19/T790M/C797S (IC50 = 6.9 nM), as well as in various ALK mutant forms, including Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM). Additionally, DA-0157 has been shown to inhibit CYP2D6 with an IC50 of 5.26 μM, and exhibits promising antitumor efficacy in preclinical mouse models, making it a valuable tool for cancer research.
DA-0157 is a selective inhibitor of the epidermal growth factor receptor (EGFR) and anaplastic lymphoma kinase (ALK), designed to address drug-resistant mutations, specifically EGFR C797S and ALK mutations in non-small cell lung cancer (NSCLC) models. It demonstrates potent antiproliferative activity in cells bearing EGFR Del19/T790M/C797S (IC50 = 6.9 nM), as well as in various ALK mutant forms, including Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM). Additionally, DA-0157 has been shown to inhibit CYP2D6 with an IC50 of 5.26 μM, and exhibits promising antitumor efficacy in preclinical mouse models, making it a valuable tool for cancer research.
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