MilliporeSigma™ Calbiochem™ Ack1 Inhibitor, AIM-100

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; 16 h 800nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC₅₀

Supplier:  MilliporeSigma™ 10483310MG

Catalog No. 10-483-310MG

Description

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; 16 h 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%; 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).

Specifications

• Color: Yellow
• Target Proteins: Ack1
• Molecular Formula: C₂₃H₂₁N₃O₂
• Solubility: DMSO
• Form: Solid

• Description: 98% by Chiral HPLC, Enantiomeric excess (ee): 98.29% (based on the ee of (S)-(+)-Tetrahydrofurfurylamine, as determined using Chiral HPLC column)
• CAS: 873305-35-2
• Formula Weight: 371.4g/mol
• Content And Storage: Avoid Freeze-Thaw Cycles, Protect from Light
• Quantity: 10 mg