Acalabrutinib [1420477-60-6]
Cat# HY-17600-100mg
Size : 100mg
Marca : MedChemExpress
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Acalabrutinib (Synonyms: ACP-196)
- Cat. No.: HY-17600 Pureté: 99.88%
- COA Instruction de manipulation
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
Size | Prix | Stock | Quantité |
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Échantillon gratuit (0.1 - 0.5 mg) | Appliquer maintenant | ||
Solid + Solvent | |||
10 mM * 1 mL
in DMSO
ready for reconstitution
|
USD 55 | En stock | |
Solution | |||
10 mM * 1 mL in DMSO | USD 55 | En stock | |
Solid | |||
5 mg | USD 50 | En stock | |
10 mg | USD 70 | En stock | |
50 mg | USD 130 | En stock | |
100 mg | USD 190 | En stock | |
200 mg | USD 290 | En stock | |
500 mg | Obtenir un devis | ||
1 g | Obtenir un devis |
* Veuillez sélectionner la quantité avant d'ajouter des articles.
This product is a controlled substance and not for sale in your territory.
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Based on 20 publication(s) in Google Scholar
Other Forms of Acalabrutinib:
- Acalabrutinib-d4 In-stock
- Acalabrutinib-d3 Obtenir un devis
20 Publications Citing Use of MCE Acalabrutinib
- •Signal Transduct Target Ther. 2020 Sep 14;5(1):200. [Abstract]
- •Cell Death Dis. 2024 Mar 18;15(3):224. [Abstract]
- •Acta Pharmacol Sin. 2020 Aug 27. [Abstract]
- •Pharmacol Res. 2020 Jan;151:104512. [Abstract]
- •Int J Biol Macromol. 2019 Apr 15;127:536-543. [Abstract]
- •Matrix Biol. 2022 Aug 25;S0945-053X(22)00104-4. [Abstract]
- •J Med Chem. 2021 Oct 21. [Abstract]
- •J Med Chem. 2019 Jul 25;62(14):6561-6574. [Abstract]
- •Pharmaceutics. 2022, 14(9), 1876.
- •Cell Signal. 2022 May 18;96:110358. [Abstract]
- •Eur J Immunol. 2021 Jul 29. [Abstract]
- •Cancers (Basel). 2020 Dec 11;12(12):3731. [Abstract]
- •Stem Cell Reports. 2019 May 14;12(5):996-1006. [Abstract]
- •Front Cardiovasc Med. 2023 Aug 15.
- •Vascul Pharmacol. 2023 Apr 17;107172. [Abstract]
- •Fundam Clin Pharmacol. 2021 Feb 1. [Abstract]
- •BMC Cancer. 2021 Jun 26;21(1):732.
- •Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11. [Abstract]
- •bioRxiv. 2023 Dec 18.
- •bioRxiv. 2023 Jul 29.
Activité biologique
Pureté et documentation
Références
Avis client
Description |
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)[1][2]. 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 & Target |
IC50: 3 nM (BTK in CD69 B cell)[2] |
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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[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Acalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activity[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Essai clinique |
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Masse moléculaire |
465.51 |
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Formule |
C26H23N7O2 |
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CAS No. | |||||||||||||
Appearance |
Solid |
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Color |
Off-white to light brown |
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SMILES |
O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C([C@H]5N(C(C#CC)=O)CCC5)=N3)C=C2 |
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Livraison | Room temperature in continental US; may vary elsewhere. |
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Stockage |
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Solvant et solubilité |
In Vitro:
DMSO : 125 mg/mL (268.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Pureté et documentation | |||||||||||||
Références |
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Complete Stock Solution Preparation Table
*
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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. 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 |
Acalabrutinib Related Classifications
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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:
- Acalabrutinib
- Cat. No.:
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