Product Data Sheet

DA-0157

Catalog No. A28802

main product photo
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.
Chemical Information
Catalog NumA28802
M. Wt656.60
FormulaC31H43BrN7O2P
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2756978-82-0
Synonyms
SMILESCN1CCN(C2CCN(C3=C(C)C=C(NC4=NC(NC5=C(P(C)(C)=O)C=C(C)C=C5)=C(Br)C=N4)C(OC)=C3)CC2)CC1
Biological Activity
DescriptionDA-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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