Description

• A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC 50 = 22nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16 h 800nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC 50 ≥346.7nM) and no inhibitory activity toward 25 other kinases
• Shown to completely inhibit EGF-induced, but not androgen DHT- (dihydrotestosterone) stimulated, AR transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures
• Effectively inhibits androgen-independent LNCaP prostate cancer growth both in vitro (by 60%; 72 h 8μM) and in castrated mice in vivo (4mg/kg/96 h injections on day 7/11/15/19/23/27 post tumor transplant).