2. Protein Tyrosine Kinase/RTK
  3. Itk
  4. ITK degrader 1

ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). 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. ITK degrader 1 also shows good plasma exposure levels.

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ITK degrader 1 Chemical Structure

ITK degrader 1 Chemical Structure

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ITK degrader 1 Related Antibodies

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Description

ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). 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. ITK degrader 1 also shows good plasma exposure levels[1].

In Vitro

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.

ITK degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.001 μM, 0.003 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time: 12 h
Result: Exhibited strong ITK degradation potencies in a dose-dependent manner. Even rapidly led to significant ITK protein downregulation after 1 h incubation.
In Vivo

ITK degrader 1 (compound 28) (20 mg/kg; ip; single dose) significantly degrades ITK protein 2 h, 8 h, and 16 h after treatment on mice. ITK degrader 1 (25 mg/kg; ip; single dose) also inhibits inhibits IL-2 secretion 6 h after treatment in vivo in anti-CD3 monoclonal antibody (mAb)-induced IL-2 mouse model[1].

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.

Animal Model: Balb/c mice, and anti-CD3 mAb-induced IL-2 mouse model[1]
Dosage: 20 mg/kg, 25 mg/kg
Administration: IP; singel dose
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.
Molecular Weight

943.02

Formula

C48H57F3N10O7
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ITK degrader 1 Related Classifications

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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.

Keywords:

ITK degrader 1ITK degrader1ITK degrader-1ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseInhibitorinhibitorinhibit

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