DA-0157

DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM) . DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models[1].

Product Specifications

CAS Number

[2756978-82-0]

UNSPSC

12352005

Target

Anaplastic lymphoma kinase (ALK) ; Cytochrome P450; EGFR

Related Pathways

JAK/STAT Signaling; Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

CN1CCN(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

Molecular Formula

C31H43BrN7O2P

Molecular Weight

656.60

References & Citations

[1]He P, et al., Discovery and preclinical evaluations of drug candidate DA-0157 capable of overcoming EGFR drug-resistant mutation C797S and EGFR/ALK co-mutations. Eur J Med Chem. 2025 Apr 5;287:117323.