1. Protein Tyrosine Kinase/RTK
  2. Btk

Acalabrutinib (Synonyms: ACP-196)

Cat. No.: HY-17600 Purity: 99.86%
Handling Instructions

Acalabrutinib is a novel, potent, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in a human whole-blood CD69 B cell activation assay.

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 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 228 In-stock
Estimated Time of Arrival: December 31
100 mg USD 408 In-stock
Estimated Time of Arrival: December 31
200 mg USD 648 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Acalabrutinib is a novel, potent, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in a human whole-blood CD69 B cell activation assay.

IC50 & Target

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

In Vitro

Acalabrutinib inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells[2].

In Vivo

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. Acalabrutinib significantly decreases tumor burden in the spleen of the mice. In the TCL1 adoptive transfer model, acalabrutinib treatment decreases phosphorylation of BTK, PLCγ2 and S6. Most notably, acalabrutinib results in a significant increase in survival compared to mice receiving vehicle[1]. 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[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)

H2O : < 0.1 mg/mL (insoluble)

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    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

  • 2.

    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

  • 3.

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

    Solubility: 2.08 mg/mL (4.47 mM); Suspended solution; Need ultrasonic and warming

References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.86%

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Product Name:
Acalabrutinib
Cat. No.:
HY-17600
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Acalabrutinib

Cat. No.: HY-17600