Acalabrutinib (Synonyms: Calquence; ACP-196)

Name: Acalabrutinib
Brand: MedChemExpress
SKU: HY-17600
Rating: 5.0 (31 reviews)

Cat. No.: HY-17600 Purity: 99.86%: Data Sheet
COA

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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 can be used for CLL research. Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

CAS No. : 1420477-60-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	Get quote
1 g	Get quote

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Based on 31 publication(s) in Google Scholar

Other Forms of Acalabrutinib:

31 Publications Citing Use of MCE Acalabrutinib

Flow Cytometry

Cell Imaging/Staining

ELISA

Histological Imaging/Staining

: Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199. [Abstract]; Aged mice were given vehicle or Acalabrutinib (0.15 mg/mL, drinking water administration) for 21 days (n = 10 per group, pooled from two experiments). Flow cytometry plots; right, FO B cell and ABCs (CD21loCD11c+) percentages among mature B cells.

: Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199. [Abstract]; Aged mice were given vehicle or Acalabrutinib (0.15 mg/mL, drinking water administration) for 7 days. Each group was tested in two experiments (n = 4 or 3 per experiment). The percentage of Ki67+ FO B cells and ABCs was compared.

: Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199. [Abstract]; Autoantibodies against histone, dsDNA, and Sm/RNP in vehicle- or Acalabrutinib (0.15 mg/mL, drinking water administration, 3 weeks)-treated mice serum were tested by enzyme-linked immunosorbent assay (ELISA). OD, optical density.

: Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199. [Abstract]; Representative renal immunostaining of immunoglobulin deposition in kidneys, stained with anti-IgG, and bright-field imaging from vehicle-treated WT and vehicle- or Acalabrutinib (0.15 mg/mL, drinking water administration, 3 weeks)-treated bm12-induced lupus mice. Scale bars, 50 μm.

: Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199. [Abstract]; Schematic for Acalabrutinib treatment from day 0. CD19+ B cells were cultured with R848, IL-21, anti-Ig, and BAFF supplemented with Acalabrutinib (10 μM, 3 days) or DMSO for 3 days. Representative flow cytometry plots of CD11c and T-bet expression in each group on day 3 and the frequency of CD11c+T-bet+ ABCs among live B cells.

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Biological Activity
Purity & Documentation
References
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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). Acalabrutinib can be used for CLL research^[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]

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	358 μM Compound: ACP-196	Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]
NAMALVA	IC₅₀	> 10 μM Compound: ACP-196	Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]
Pfeiffer	IC₅₀	> 10 μM Compound: ACP-196	Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]
Raji	IC₅₀	> 10 μM Compound: ACP-196	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]
Ramos	IC₅₀	31.3 μM Compound: ACP-196	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]
Rec1	IC₅₀	0.013 μM Compound: ACP-196	Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]
SU-DHL-2	IC₅₀	> 10 μM Compound: ACP-196	Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]
TMD8	IC₅₀	0.014 nM Compound: Acalabrutinib	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 33740548]
TMD8	IC₅₀	0.024 μM Compound: ACP-196	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34672559]

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].
Acalabrutinib inhibits purified BTK with an IC₅₀ of 3 nM and an EC₅₀ of 8 nM in a human whole-blood CD69 B cell activation assay. Acalabrutinib has improved target specificity over ibrutinib with 323-, 94-, 19-, and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC , respectively) and no activity against EGFR^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

465.51

Formula

C₂₆H₂₃N₇O₂

CAS No.

1420477-60-6

Appearance

Solid

Color

Off-white to light brown

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 116.67 mg/mL (250.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1482 mL	10.7409 mL	21.4818 mL
5 mM	0.4296 mL	2.1482 mL	4.2964 mL
10 mM	0.2148 mL	1.0741 mL	2.1482 mL

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.
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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

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

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

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.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (280 KB) SDS (396 KB)

COA (257 KB) Elemental Analysis Report (115 KB)

Handling Instructions (2659 KB)

References

[1]. Wu J, et al. Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor. J Hematol Oncol. 2016 Mar 9;9:21 [Content Brief]

[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 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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

Help & FAQs

Do most proteins show cross-species activity?
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.

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Acalabrutinib (Synonyms: Calquence; ACP-196)

Customer Review

Other Forms of Acalabrutinib:

Acalabrutinib Related Antibodies

31 Publications Citing Use of MCE Acalabrutinib

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•Related Screening Libraries:

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Biological Activity

Purity & Documentation

References

Customer Review

Acalabrutinib Related Antibodies

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Complete Stock Solution Preparation Table

Acalabrutinib Related Classifications

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