VAV1 degrader-3

Cat. No.: HY-168625 Purity: 99.26%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC₅₀: 7 nM). VAV1 degrader-3 reduces immune cell activation, immune cell proliferation and the production of various cytokines. VAV1 degrader-3 can be used for research of inflammatory or autoimmune disorder. VAV1 degrader-3 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc..

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

VAV1 degrader-3 Chemical Structure

CAS No. : 3050683-38-7

Size		Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution		Check price and availability
Solution
10 mM * 1 mL in DMSO		Check price and availability
Solid
5 mg		Check price and availability
10 mg		Check price and availability
25 mg		Check price and availability
50 mg		Check price and availability

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

VAV1 degrader-3 (0-1 μM, 24 h) inhibtis B cell receptor-mediated activity, specifically, VAV1 degrader-3 inhibits CD69 expression, and IL-6, lgG secretion in PBMC cells isolated from human blood leukopaks^[1].
VAV1 degrader-3 (0-1 μM, 24 h) inhibits T cell receptor-mediated CD69 activation, IL-2 secretion, and proliferation of Primary T-cells^[1].

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

In Vivo

VAV1 degrader-3 (1-15 mg/kg, p.o.) inhibits disease progression in MOGss-ss-induced multiple sclerosis experimntal autoimmune encephalomyelitis (EAE) mouse model^[1].
VAV1 degrader-3 (1 mg/kg, p.o.) inhibits disease progression and reduces expression of calprotectin subunits (S100a8/S100a9) within colon tissue in a T cell transfer-induced model of colitis^[1].
VAV1 degrader-3 (1 mg/kg, p.o.) also inhibits disease progression collagen-induced arthritis (CIA) mouse model^[1].

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

Molecular Weight

392.83

Formula

C₂₂H₁₇ClN₂O₃

CAS No.

3050683-38-7

Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C2CCC(NC2=O)=O)C=CC=C1C3=CC=C(N4C(C=CC=C4)=O)C=C3

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 : 100 mg/mL (254.56 mM; ultrasonic and warming and heat to 60°C; 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	2.5456 mL	12.7282 mL	25.4563 mL
5 mM	0.5091 mL	2.5456 mL	5.0913 mL
10 mM	0.2546 mL	1.2728 mL	2.5456 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.26%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (249 KB) HNMR (143 KB) RP-HPLC (163 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

References

[1]. Laura Ann Mcallister, et al. Targeted degradation of vav1. Patent. WO2024151547A1.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5456 mL	12.7282 mL	25.4563 mL	63.6408 mL
	5 mM	0.5091 mL	2.5456 mL	5.0913 mL	12.7282 mL
	10 mM	0.2546 mL	1.2728 mL	2.5456 mL	6.3641 mL
	15 mM	0.1697 mL	0.8485 mL	1.6971 mL	4.2427 mL
	20 mM	0.1273 mL	0.6364 mL	1.2728 mL	3.1820 mL
	25 mM	0.1018 mL	0.5091 mL	1.0183 mL	2.5456 mL
	30 mM	0.0849 mL	0.4243 mL	0.8485 mL	2.1214 mL
	40 mM	0.0636 mL	0.3182 mL	0.6364 mL	1.5910 mL
	50 mM	0.0509 mL	0.2546 mL	0.5091 mL	1.2728 mL
	60 mM	0.0424 mL	0.2121 mL	0.4243 mL	1.0607 mL
	80 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7955 mL
	100 mM	0.0255 mL	0.1273 mL	0.2546 mL	0.6364 mL

VAV1 degrader-3 Related Classifications

Inflammation/Immunology

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:

VAV1 degrader-33050683-38-7Molecular GluesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

VAV1 degrader-3

VAV1 degrader-3 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

VAV1 degrader-3 Related Antibodies

Molarity Calculator

Dilution Calculator