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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
A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22 nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16 h 800 nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥346.7 nM) 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 8 µM) and in castrated mice in vivo (4 mg/kg/96 h injections on day 7/11/15/19/23/27 post tumor transplant).
产品信息
Form Yellow solid
Primary Target Ack1
Primary Target IC50 22 nM for Ack1
Secondary target Lck, Lyn
Molar mass 371.4
Protect from Light 是的
Avoid freeze/thaw 是的
Packaged under inert gas 是的
Cell permeable 是的
Reversible 是的
Purity ≥98% by Chiral HPLC
Enantiomeric excess (ee): 98.29% (based on the ee of (S)-(+)-Tetrahydrofurfurylamine, as determined using Chiral HPLC column)
Solubility DMSO
Chemical formula C23H21N3O2
CAS number 873305-35-2
商店和运输信息
Storage -20°C
Ship Ambient Temperature Only
Standard Handling |