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An inhibitor of Src kinase, binds to Src (Kd = 315 nM), decreases phosphorylation at the Y416 activation site, and increases phosphorylation at the Y527 inactivation site, reduces the proliferation of wild-type NCI H358 cells and KRASG12C-expressing NCI H358 cells (IC50s = 2.14 and 2.03 µM, respectively), inhibits migration and invasion of NCI H358 cells at 2, 4, and 8 µM, induces cell cycle arrest in the G2/M phase at 1, 4, and 8 µM, and induces apoptosis at 4 and 8 µM, reduces tumor volume in an NCI H358 mouse xenograft model at 25, 50, and 100 mg/kg. Formulation: A crystalline solid. InChI: InChI=1S/C18H16N2O2/c1-21-14-8-10-18(22-2)13(11-14)7-9-17-15-5-3-4-6-16(15)19-12-20-17/h3-12H,1-2H3/b9-7+. InChIKey: BZIBNGDUNNRTCZ-VQHVLOKHSA-N. SMILES: COC1=CC(/C=C/C2=NC=NC3=CC=CC=C23)=C(OC)C=C1
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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