TX1-85-1

TX1-85-1 is an inhibitor of the epidermal growth factor receptor tyrosine kinase ErbB3 (IC50 = 23 nM). It also binds to ErbB2, Lyn, and several other Src family kinases in a live cell chemical proteomics assay when used at a concentration of 2 µM. TX1-85-1 inhibits phosphorylation of Akt and ERK1/2 in ErbB3-dependent HCC2935 and OVCAR-8 cells when used at concentrations of 5 and 2 µM, respectively. However, it does not inhibit proliferation of ErbB3-dependent PC9 GR4, HCC827 GR8, or OVCAR-8 cells (EC50s = >10 µM).Formal Name: N-[5-[1-[4-(4-acetyl-1-piperazinyl)cyclohexyl]-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-phenoxyphenyl]-2-propenamide. CAS Number: 1603845-32-4. Molecular Formula: C32H36N8O3. Formula Weight: 580.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.2 mg/ml, DMSO: 0.2 mg/ml. lambdamax: 266 nm. SMILES: O=C(C=C)NC1=CC(C2=NN(C3CCC(N4CCN(C(C)=O)CC4)CC3)C5=NC=NC(N)=C52)=CC=C1OC6=CC=CC=C6. InChi Code: InChI=1S/C32H36N8O3/c1-3-28(42)36-26-19-22(9-14-27(26)43-25-7-5-4-6-8-25)30-29-31(33)34-20-35-32(29)40(37-30)24-12-10-23(11-13-24)39-17-15-38(16-18-39)21(2)41/h3-9,14,19-20,23-24H,1,10-13,15-18H2,2H3,(H,36,42)(H2,33,34,35). InChi Key: FYICDSWKKFSYOM-UHFFFAOYSA-N.