85-2071-02　Ack1 Inhibitor, AIM-100 (Activated Cdc42 Kinase 1 Inhibitor, (S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine) 10mg　217139

特徴

• A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16h 800nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥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%; 72h 8uM) and in castrated mice in vivo (4mg/kg/96h injections on day 7/11/15/19/23/27 post tumor transplant).
• Formula:C23H21N3O2
• Solubility:DMSO
• Primary Target:Ack1
• Primary Target IC50:22nM for Ack1
• Secondary Target:Lck, Lyn
• Molar Mass:371.4
• Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months after receipt at -20°C. Reconstitute with sterile buffer or ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.