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
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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