Art. -Nr.: HY-109078

Vecabrutinib

(Synonyms: SNS-062)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with K_d values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC₅₀ of 24 nM for ITK.

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Reinheit: 99.76%
CAS. Nr.: 1510829-06-7
Formel: C₂₂H₂₄ClF₄N₇O₂
Molecular Weight:529.92

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Vecabrutinib Chemical Structure

CAS. Nr.: 1510829-06-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with K_d values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC₅₀ of 24 nM for ITK^[1]^[2].

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 PCI-32765 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 PCI-32765 via immunoblot for BTK phosphorylation. Vecabrutinib decreases viability of primary CLL cells in the presence of HS5 stromal protection by 5.5%^[2].

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

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 PCI-32765^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1510829-06-7
Appearance Solid
Molecular Weight 529.92
Formel C₂₂H₂₄ClF₄N₇O₂
Color White to light yellow
SMILES

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

SNS-062
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (3)

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Journal Impact Factor

Proc Natl Acad Sci U S A

Endocytosis triggers V-ATPase-SYK-mediated priming of cGAS activation and innate immune response. [Abstract]

2022 Oct 25;119(43):e2207280119. PMID: 36252040
Blood Adv

PLCG2 Exon-Skipped Variants: Insights into Their Potential Role in Chronic Lymphocytic Leukemia. [Abstract]

2026 Jun 5:bloodadvances.2025019077. PMID: 42263669
JCI Insight

Noncovalent inhibitors reveal BTK gatekeeper and auto-inhibitory residues that control its transforming activity. [Abstract]

2019 Jun 20;4(12):e127566. PMID: 31217352

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (235.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.72 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.72 mM); Clear solution

Protocol 3

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

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.

Protocol 4

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

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.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.93 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Minke E. Binnerts, et al. Abstract C186: SNS-062 is a potent noncovalent BTK inhibitor with comparable activity against wild type BTK and BTK with an acquired resistance mutation. Molecular Cancer Therapeutics. December 2015 Volume 14, Issue 12 Supplement 2

[2]. Catherine A. Fabian, et al. Abstract 1207: SNS-062 demonstrates efficacy in chronic lymphocytic leukemia in vitro and inhibits C481S mutated Bruton tyrosine kinase. Cancer Research July 2017 Volume 77, Issue 13 Supplement

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8871 mL	9.4354 mL	18.8708 mL	47.1769 mL
	5 mM	0.3774 mL	1.8871 mL	3.7742 mL	9.4354 mL
	10 mM	0.1887 mL	0.9435 mL	1.8871 mL	4.7177 mL
	15 mM	0.1258 mL	0.6290 mL	1.2581 mL	3.1451 mL
	20 mM	0.0944 mL	0.4718 mL	0.9435 mL	2.3588 mL
	25 mM	0.0755 mL	0.3774 mL	0.7548 mL	1.8871 mL
	30 mM	0.0629 mL	0.3145 mL	0.6290 mL	1.5726 mL
	40 mM	0.0472 mL	0.2359 mL	0.4718 mL	1.1794 mL
	50 mM	0.0377 mL	0.1887 mL	0.3774 mL	0.9435 mL
	60 mM	0.0315 mL	0.1573 mL	0.3145 mL	0.7863 mL
	80 mM	0.0236 mL	0.1179 mL	0.2359 mL	0.5897 mL
	100 mM	0.0189 mL	0.0944 mL	0.1887 mL	0.4718 mL

Keywords

Vecabrutinib

3 Cited Publications

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Vecabrutinib

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Publications Citing Use of MedChemExpress (MCE) Vecabrutinib

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vecabrutinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Autoimmune Disease Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Vecabrutinib

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vecabrutinib Related Classifications

HY-109078 Related Classifications