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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C48H57F3N10O7
- 分子量:943.02
-
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
体外実験
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. .
-
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.
体内実験
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.
化学情報
-
分子量 943.02
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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)
PROTAC ITK degrader 1 関連分類
HY-149917 関連分類
Powered by Bioz