Synonyms: A 770041; A770041; 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; trans-KIN 001-111
Molecular Formula: C34H39N9O3
Molecular Weight: 621.73
Linear Structural Formula: C34H39N9O3
MDL Number: MFCD24873124
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: A-770041 is an orally available (rat F = 34.1%; 10 mg/kg p.o.), ATP-competitive, potent and selctive Lck inhibtor (IC50 = 147 nM/Lck, 1.18 muM/Lyn, 1.22 muM/Hck, 9.05 muM/Src, 14.1 muM/Fgr, 44.1 muM/Fyn; >25 muM/IKK1, IKK2, IRAK4, p38, JAK3, ZAP70, ITK, PKC, MK2, PKA, TYK2, COT,Syk; >50 muM/Tie-2 & Kdr; 1 mM ATP). A-770041 inhibits CD3 mAb-induced IL-2 production in human whole blood in vitro (IC 50 = 80 nM) and in mice in vivo (IC50 = 78 nM plasma conc.), and significantly lengthens graft survival time in a rat heterotopic heart transplant model (2.5 & 5 mg/kg bid p.o.).