1. Protein Tyrosine Kinase/RTK
  2. Btk
    Itk

Vecabrutinib (Synonyms: SNS-062)

Cat. No.: HY-109078 Purity: 99.96%
Handling Instructions

Vecabrutinib is a potent, noncovalent BTK and ITK inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively; Vecabrutinib shows an IC50 of 24 nM for ITK.

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

Vecabrutinib Chemical Structure

Vecabrutinib Chemical Structure

CAS No. : 1510829-06-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 525 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Vecabrutinib is a potent, noncovalent BTK and ITK inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively; Vecabrutinib shows an IC50 of 24 nM for ITK.

IC50 & Target

IC50: 24 nM (ITK)[2]
Kd: 0.3 nM (BTK), 2.2 nM (ITK)[1]

In Vitro

Vecabrutinib inhibits pBTK in human whole blood with an average IC50 of 50 nM. Vecabrutinib inhibits WT and C481S BTK with similar IC50s (pBTK IC50s: WT BTK 2.9 nM, C481S BTK 4.4 nM)[1]. In a recombinant kinase assay, IC50s of Vecabrutinib against WT BTK and C481S BTK are 4.6 nM and 1.1 nM. Vecabrutinib retains activity against the mutated BTK variant. Vecabrutinib is six times more potent than ibrutinib and greater than 640 times more potent than acalabrutinib against C481S BTK. Vecabrutinib demonstrates dose-dependent inhibition of BTK in primary patient CLL cells comparable to ibrutinib via immunoblot for BTK phosphorylation. Vecabrutinib decreases viability of primary CLL cells in the presence of HS5 stromal protection by 5.5%[2].

In Vivo

Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours. Vecabrutinib is well tolerated with continuous drug levels and at exposures much greater than those achieved for ibrutinib[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (235.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8871 mL 9.4354 mL 18.8708 mL
5 mM 0.3774 mL 1.8871 mL 3.7742 mL
10 mM 0.1887 mL 0.9435 mL 1.8871 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution

References
Molecular Weight

529.92

Formula

C₂₂H₂₄ClF₄N₇O₂

CAS No.

1510829-06-7

SMILES

NC([[email protected]@H]1[[email protected]@H](N(CCC[[email protected]]2NC3=CC(C(F)(F)F)=CC(Cl)=C3)C2=O)CN(C4=NC=NC(N)=C4F)CC1)=O

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: 99.96%

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Product Name:
Vecabrutinib
Cat. No.:
HY-109078
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Vecabrutinib

Cat. No.: HY-109078