DA-0157 - CAS 2756978-82-0

DA-0157 is an orally active inhibitor targeting EGFR and ALK, designed to overcome resistance mutations in non-small cell lung cancer (NSCLC) . It effectively 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) . Additionally, DA-0157 inhibits CYP2D6 with an IC50 of 5.26 μM and demonstrates antitumor activity in mouse models.

ALK, Cytochromes P450, EGFR

Tyrosine Kinase/Adaptors, Metabolism, JAK/STAT signaling, Angiogenesis

2756896

C31H43BrN7O2P

656.597

O=P(C1=CC(=CC=C1NC2=NC(=NC=C2Br)NC=3C=C(C(=CC3OC)N4CCC(N5CCN(C)CC5)CC4)C)C)(C)C

-20°C

Ice Packs

Small Compound