ITK-IN-7
ITK-IN-7 is a selective ITK inhibitor with an IC50 of 16 nM and a Ki of 0.48 nM. ITK-IN-7 reduces IL-2 secretion levels in T cells and in mouse models stimulated by anti-CD3 monoclonal antibodies. ITK-IN-7 can be used for basic and translational research related to ITK inhibition, such as research on leukemia.
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- CAS 番号: 3126105-55-0
- 分子式: C27H35N7O2
- 分子量:489.61
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
ITK-IN-7 (compound 19) (1 μM) potently inhibits ITK and exhibits exceptional selectivity over 24 other tested kinases, including BTK and key TCR pathway kinases[1].
ITK-IN-7 inhibits recombinant BTK kinase activity with an IC50 of 5059 nM, representing over 300-fold selectivity for ITK over BTK[1].
ITK-IN-7 (0.01-10 μM; 4 h) potently inhibits PLCγ1 phosphorylation in Jurkat cells with an EC50 of 15 nM and dose-dependently inhibits ERK phosphorylation[1].
ITK-IN-7 (3 μM; 4 h) induces sustained inhibition of PLCγ1 phosphorylation in Jurkat cells for over 12 h post-washout[1].
ITK-IN-7 (range of concentrations; 4 h pretreatment, 24 h stimulation) potently inhibits IL-2 secretion in TCR-stimulated Jurkat cells with an EC50 of 19 nM[1].
ITK-IN-7 (range of concentrations; 72 h) inhibits proliferation of Jurkat, MOLT-4, and CCRF-CEM T-cell leukemia cells with GI50 values of 0.8 μM, 3.4 μM, and 2.6 μM, respectively, and exhibits reduced activity against B-cell lines and non-malignant HEK293T cells[1].
ITK-IN-7 (0.03-10 μM) does not inhibit BTK-mediated PLCγ2 phosphorylation in Namalwa B cells, confirming excellent cellular selectivity for ITK over BTK[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Parmacokinetics
| Species | Dose | Route | C0 | T1/2 | AUC0-t | AUC0-∞ | Vz | CL | Vss | MRT |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.p. | 3473 ng/mL | 2.19 h | 555 ng·h/mL | 561 ng·h/mL | 11.6 L/kg | 62.7 mL/min/kg | 2.51 L/kg | 0.53 h |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:i.p.; single dose
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Result:Reduced serum IL-2 levels by nearly 50% compared to the vehicle group when measured 3 hours post-dose at 50 mg/kg.
Reduced serum IL-2 levels by approximately 80% compared to the vehicle group when measured 3 hours post-dose at 100 mg/kg.
Maintained over 70% IL-2 suppression when measured 8 hours post-dose at 100 mg/kg.
化学情報
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CAS 番号 3126105-55-0
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分子量 489.61
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分子式 C27H35N7O2
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SMILES
O=C(C1=NNC2=C1CCC(C)(C)C2)NC3=CN([C@H](C4=CC=CC=C4)CCN(C)C)N=C3NC(C=C)=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)
ITK-IN-7 関連分類
HY-184275 関連分類
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