DA-0157

• Description :

  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].

• 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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [2756978-82-0]