PROTAC ITK degrader 1
PROTAC ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. PROTAC ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo.
(Pink: Itk ligand (HY-168387); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168388)).
For research use only. We do not sell to patients.
- Formula: C48H57F3N10O7
- Molecular Weight:943.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
PROTAC ITK degrader 1 (compound 28) (0.001-3 μM; 12 h) dose-dependently decreases the protein levels of ITK in Jurkat cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat cells
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Concentration:0.001 μM, 0.003 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
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Incubation Time:12 h
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Result:Exhibited strong ITK degradation potencies in a dose-dependent manner. Even rapidly led to significant ITK protein downregulation after 1 h incubation.
Pharmacokinetic Analysis in Balb/c Mice[1]
| Route | Dose (mg/kg) | AUC0-t (ng·h/mL) | AUC0-∞ (ng·h/mL) | T1/2 (h) | Vz (L/kg) | Cl (mL/min/kg) | Cmax (ng/mL) | MRTlast (h) | Bioavailability (%) |
| i.v. | 5 | 15138 | 15415 | 4.39 | 2057 | 5.4 | 4910 | 4.42 | / |
| ip | 10 | 25931 | 27261 | 5.75 | 3055 | 6.1 | 3423 | 5.84 | 88.4% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice, and anti-CD3 mAb-induced IL-2 mouse model[1]
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Dosage:20 mg/kg, 25 mg/kg
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Administration:IP; singel dose
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Result:Successfully delivered to the peripheral blood and spleen tissue, eliciting efficient, rapid, and prolonged ITK degradation starting at 2 h and lasting for at least 16 h with 20 mg/kg dose in Balb/c mice.
Efficiently suppressed the production of cytokine IL-2, resulting in a reduction of over 70% compared to the vehicle group with 25 mg/kg dose.
Chemical Information
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Molecular Weight 943.02
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Formula C48H57F3N10O7
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SMILES
O=C(NC1=CN([C@@H](CCN2CCN(CCC3CCN(C4=CC=C(C(N(C5CCC(NC5=O)=O)C6=O)=O)C6=C4)CC3)CC2)C7=CC=CC=C7)N=C1)C8=NNC9=C8CCC(C)(C)C9.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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