K882

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