1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Acalabrutinib

Acalabrutinib (Synonyms: ACP-196)

Cat. No.: HY-17600 Purity: 99.94%
Handling Instructions

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).

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

Acalabrutinib Chemical Structure

Acalabrutinib Chemical Structure

CAS No. : 1420477-60-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 130 In-stock
Estimated Time of Arrival: December 31
100 mg USD 190 In-stock
Estimated Time of Arrival: December 31
200 mg USD 290 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target

IC50: 3 nM (BTK in CD69 B cell)[2]

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].

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].

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

Clinical Trial
Molecular Weight

465.51

Formula

C₂₆H₂₃N₇O₂

CAS No.

1420477-60-6

SMILES

O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C([[email protected]]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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (268.52 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.25 mg/mL (4.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.25 mg/mL (4.83 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.25 mg/mL (4.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.94%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

AcalabrutinibACP-196ACP196ACP 196BtkBruton tyrosine kinaseorallyirreversibletyrosinephosphorylationERKIKBAKTCLLCys481on-targetchroniclymphocyticleukemiaPLCγ2Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Acalabrutinib
Cat. No.:
HY-17600
Quantity:
MCE Japan Authorized Agent: