Acalabrutinib-ACP-196-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAcalabrutinibCat. No.: HY-17600CAS No.: 1420477-60-6Synonyms: ACP-196分式: CHNO分量: 465.51作靶点: Btk作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (268

2、.52 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (4.83 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.25 mg/mL (4.83 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.25 mg/mL (4

3、.83 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Acalabrutinib种新颖的，有效的，选择性的 BTK 抑制剂，在体内试验中 IC50 和 EC50 分别为 3 nM 和 8nM。IC50 & Target IC50: 3 nM (BTK in CD69 B cell) 2体外研究 Acalabrutinib inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitrosignaling assay on primary

4、 human CLL cells 2.体内研究 In the human CLL NSG xenograft model, acalabrutinib demonstrates on-target effects including decreasedphosphorylation of PLC2, ERK and significant inhibition of CLL cell proliferation. Acalabrutinib significantlydecreases tumor burden in the spleen of the mice. In the TCL1 ad

5、optive transfer model, acalabrutinibtreatment decreases phosphorylation of BTK, PLC2 and S6. Most notably, acalabrutinib results in asignificant increase in survival compared to mice receiving vehicle 1. Acalabrutinib (100 mg twice per day)assessed for thrombus formation at injured arterioles of the

6、 mice, exhibits more selective for inhibiting BTKand has virtually no inhibition of platelet activity 2.户使本产品发表的科研献 J Med Chem. 2019 Jul 1. Stem Cell Rep. 2019 Apr. Int J Biol Macromol. 2019 Apr 15;127:536-543.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Herman SE, et al. Th

7、e Brutons tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in twomouse models of chronic lymphocytic leukemia. Clin Cancer Res. 2016 Nov 302. Wu J, et al. Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor. J Hematol Oncol. 2016 Mar 9;9:21McePdfHeightCaution: Product has not been fully validated for medical applications.For research u