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.
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- CAS 番号: 3119457-09-6
- 分子式: C23H17ClF2N2O4
- 分子量:458.84
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
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
体内実験
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.
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Animal Model:ICR mice (male; healthy)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Showed a Cmax of 2970 ng/mL and an AUC0-t of 37623 h·ng/mL in male ICR mice.
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Animal Model:SD rats (180-240 g; male; healthy)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Showed a Cmax of 15467 ng/mL and an AUC0-t of 176412 h·ng/mL.
化学情報
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CAS 番号 3119457-09-6
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分子量 458.84
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分子式 C23H17ClF2N2O4
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)