Acalabrutinib [1420477-60-6]
Référence HY-17600-1ml
Conditionnement : 10mM/1mL
Marque : MedChemExpress
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Acalabrutinib Chemical Structure
CAS No. : 1420477-60-6
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Activité biologique
Pureté et documentation
Références
Avis client
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | IC50: 3 nM (BTK in CD69 B cell) |
In Vitro | Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells. In the human CLL NSG xenograft model, Acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferation. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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[1]. Wu J, et al. Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor. J Hematol Oncol. 2016 Mar 9;9:21
[2]. Herman SE, et al. The Bruton's tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia. Clin Cancer Res. 2016 Nov 30
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.1482 mL | 10.7409 mL | 21.4818 mL | 53.7045 mL |
5 mM | 0.4296 mL | 2.1482 mL | 4.2964 mL | 10.7409 mL | |
10 mM | 0.2148 mL | 1.0741 mL | 2.1482 mL | 5.3705 mL | |
15 mM | 0.1432 mL | 0.7161 mL | 1.4321 mL | 3.5803 mL | |
20 mM | 0.1074 mL | 0.5370 mL | 1.0741 mL | 2.6852 mL | |
25 mM | 0.0859 mL | 0.4296 mL | 0.8593 mL | 2.1482 mL | |
30 mM | 0.0716 mL | 0.3580 mL | 0.7161 mL | 1.7902 mL | |
40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3426 mL | |
50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0741 mL | |
60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8951 mL | |
80 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL | |
100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5370 mL |
- Protein Tyrosine Kinase/RTK
- Btk
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Acalabrutinib1420477-60-6ACP-196ACP196ACP 196BtkBruton tyrosine kinaseorallyirreversibletyrosinephosphorylationERKIKBAKTCLLCys481on-targetchroniclymphocyticleukemiaPLCγ2Inhibitorinhibitorinhibit
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- Nom du produit:
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