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  3. VAV1 degrader-4

VAV1 degrader-4 is a VAV1 molecular glue degrader with a DC50 value of 3.93 nM for VAV1 in Jurkat cells. VAV1 degrader-4 can dose-dependently inhibit the production of IL-2. VAV1 degrader-4 can be used for research on autoimmune diseases.

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

VAV1 degrader-4

VAV1 degrader-4 Chemical Structure

CAS No. : 3119457-09-6

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Description

VAV1 degrader-4 is a VAV1 molecular glue degrader with a DC50 value of 3.93 nM for VAV1 in Jurkat cells. VAV1 degrader-4 can dose-dependently inhibit the production of IL-2. VAV1 degrader-4 can be used for research on autoimmune diseases[1].

In Vitro

VAV1 degrader-4 (Compound 2) (0.24-1000 nM; 24 h) shows a DC50 value of 3.93 nM for VAV1 protein in Jurkat cells[1].
VAV1 degrader-4 (72 h) dose-dependently inhibits CD3/CD28-induced IL-2 secretion from human T cells, with an IC50 value of 0.53 nM[1].

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

Parmacokinetics
Species Dose Route Cmax AUC0-t
Mice[1] 10 mg/kg p.o. 2970 ng/mL 37623 ng·h/mL
Rat[1] 10 mg/kg p.o. 15467 ng/mL 176412 ng·h/mL
In Vivo

VAV1 degrader-4 (Compound 2) (10 mg/kg; p.o.; single dose) shows a Cmax of 2970 ng/mL and an AUC0-t of 37623 h·ng/mL in male ICR mice[1].
VAV1 degrader-4 (10 mg/kg; p.o.; single dose) shows a Cmax of 15467 ng/mL and an AUC0-t of 176412 h·ng/mL in male SD rats[1].

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

Animal Model: ICR mice (male; healthy)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Showed a Cmax of 2970 ng/mL and an AUC0-t of 37623 h·ng/mL in male ICR mice.
Animal Model: SD rats (180-240 g; male; healthy)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Showed a Cmax of 15467 ng/mL and an AUC0-t of 176412 h·ng/mL.
Molecular Weight

458.84

Formula

C23H17ClF2N2O4

CAS No.
SMILES

O=C1NC(C(CC1)C2=CC=CC(C3=CC=C(N4C=CC=C(C4=O)OC(F)F)C=C3)=C2Cl)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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Product Name:
VAV1 degrader-4
Cat. No.:
HY-182765
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