Tucatinib

Tucatinib is an inhibitor of HER2 (IC50 = 14 nM). It inhibits the phosphorylation of HER2 in BT474 breast carcinoma cells (IC50 = 21 nM). Tucatinib inhibits phosphorylation of AKT and induces apoptosis in BT474 cells. In vivo, tucatinib (25-100 mg/kg) inhibits tumor growth in NCI N87 gastric carcinoma and SKOV3 ovarian adenocarcinoma mouse xenograft models. Tucatinib also reduces intratumor phosphorylation of AKT and ERK and inhibits tumor growth in a BT474 mouse xenograft model.Formal Name: N6-(4,5-dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine. CAS Number: 937263-43-9. Synonyms: ARRY-380, ONT-380. Molecular Formula: C26H24N8O2. Formula Weight: 480.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 214, 244 nm. SMILES: CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5. InChi Code: InChI=1S/C26H24N8O2/c1-16-10-17(5-7-22(16)36-19-8-9-34-23(12-19)28-15-30-34)31-24-20-11-18(4-6-21(20)27-14-29-24)32-25-33-26(2,3)13-35-25/h4-12,14-15H,13H2,1-3H3,(H,32,33)(H,27,29,31). InChi Key: SDEAXTCZPQIFQM-UHFFFAOYSA-N.