Vecabrutinib (Synonyms: SNS-062)

Name: Vecabrutinib
Brand: MedChemExpress
SKU: HY-109078
Rating: 5.0 (2 reviews)

Cat. No.: HY-109078 Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Vecabrutinib Chemical Structure

CAS No. : 1510829-06-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 373	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 373	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 530	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 870	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1180	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1620	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Vecabrutinib

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Purity & Documentation
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Description

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

Molecular Weight

529.92

Formula

C₂₂H₂₄ClF₄N₇O₂

CAS No.

1510829-06-7

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

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

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, 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.

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: 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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 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

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: 99.76%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (252 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[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

Complete Stock Solution Preparation Table

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

Vecabrutinib 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.

Keywords:

Vecabrutinib1510829-06-7SNS-062SNS062SNS 062BtkItkBruton tyrosine kinaseInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseInhibitorinhibitorinhibit

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Vecabrutinib (Synonyms: SNS-062)

Customer Review

Vecabrutinib Related Antibodies

2 Publications Citing Use of MCE Vecabrutinib

Featured Recommendations

•Related Screening Libraries:

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•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Vecabrutinib Related Antibodies

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Complete Stock Solution Preparation Table

Vecabrutinib Related Classifications

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