A-770041

A-770041 is an inhibitor of LCK kinase (IC50 = 0.147 µM). It is selective for LCK over other Src family tyrosine kinases including Src, Fyn, Fgr, HCK, and Tie2 (IC50s = 9.05, 44.1, 14.1, 1.22, and >50 µM, respectively). A-770041 induces dephosphorylation of LCK by SHP-1, inactivating LCK, in IgE/antigen-stimulated bone marrow-derived mast cells (BMMCs). It inhibits IL-2 production induced by an anti-CD3 antibody and phorbol 12-myristate 13-acetate (PMA, Cay-10008014) in isolated human whole blood (EC50 = 80 nM) and by concanavalin A (Cay-14951) in rats. A-770041 (10 mg/kg) prevents acute rejection and increases graft survival in a rat model of heterotopic heart transplantation. It also inhibits the growth of CTV-1 human acute myeloid leukemia cells (IC50 = 224 nM) and sensitizes U2OSMR and KHOSR2 multidrug resistant human osteosarcoma cells to paclitaxel (Cay-10461) and doxorubicin (Cay-15007).Formal Name: N-[4-[1-[trans-4-(4-acetyl-1-piperazinyl)cyclohexyl]-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-1-methyl-1H-indole-2-carboxamide. CAS Number: 869748-10-7. Molecular Formula: C34H39N9O3. Formula Weight: 621.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: 0.1 M HCl: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 2 mg/ml. SMILES: NC1=C2C(C3=CC(OC)=C(C=C3)NC(C4=CC5=CC=CC=C5N4C)=O)=NN([C@@]6([H])CC[C@@](N7CCN(CC7)C(C)=O)([H])CC6)C2=NC=N1. InChi Code: InChI=1S/C34H39N9O3/c1-21(44)41-14-16-42(17-15-41)24-9-11-25(12-10-24)43-33-30(32(35)36-20-37-33)31(39-43)23-8-13-26(29(19-23)46-3)38-34(45)28-18-22-6-4-5-7-27(22)40(28)2/h4-8,13,18-20,24-25H,9-12,14-17H2,1-3H3,(H,38,45)(H2,35,36,37)/t24-,25-. InChi Key: ZMNWFTYYYCSSTF-SOAUALDESA-N.