PCI-29732

PCI-29732 is a multi-kinase inhibitor. It inhibits the Tec family kinase BTK and the Src family kinases LCK and LYN (Kis = 8.2, 4.6, and 2.5 nM, respectively), as well as the activity of three receptor tyrosine kinases and seven non-receptor tyrosine kinases by greater than 90% in a panel of over 100 kinases at 10 µM. PCI-29732 inhibits calcium flux in Ramos B cells and phosphorylation of phospholipase C?1 (PLC?1) with IC50 values of 0.53 and 0.33 µM, respectively. It is cytotoxic to S1-MI-80, H460/MX20, and KBv200 cancer cells overexpressing the ATP-binding cassette transporter (IC50s = 7.8, 6.3, and 6.02 µM, respectively). PCI-29732 (20 mg/kg), in combination with the DNA topoisomerase I inhibitor topotecan (Cay-14129), reduces tumor growth in an H460/MX20 mouse xenograft model.Formal Name: 1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine. CAS Number: 330786-25-9. Molecular Formula: C22H21N5O. Formula Weight: 371.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml, DMSO: 10 mg/ml, Ethanol: 5 mg/ml. lambdamax: 262, 289 nm. SMILES: NC1=C(C(C2=CC=C(OC3=CC=CC=C3)C=C2)=NN4C5CCCC5)C4=NC=N1. InChi Code: InChI=1S/C22H21N5O/c23-21-19-20(26-27(16-6-4-5-7-16)22(19)25-14-24-21)15-10-12-18(13-11-15)28-17-8-2-1-3-9-17/h1-3,8-14,16H,4-7H2,(H2,23,24,25). InChi Key: GMJUPMONHWAZCP-UHFFFAOYSA-N.