| Bioactivity | 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]. |
| Invitro | ITK degrader 1 (compound 28) (0.001-3 μM；12 小时) 剂量依赖性地降低 Jurkat 细胞中的 ITK 蛋白水平[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | ITK degrader 1 (compound 28) (20 mg/kg；腹腔注射；单剂量) 在处理小鼠后 2 小时、8 小时和 16 小时显着降解 ITK 蛋白。 在抗 CD3 单克隆抗体 (mAb) 诱导的 IL-2 小鼠模型中，ITK degrader 1 处理 6 小时后，(25 mg/kg；腹腔注射；单剂量) 也抑制 IL-2 分泌[1]。在 Balb/c 小鼠中的药代动力学分析[1]Route |
| Name | ITK degrader 1 |
| Formula | C48H57F3N10O7 |
| Molar Mass | 943.02 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhou D, et al. Discovery of Potent and Highly Selective Interleukin-2-Inducible T-Cell Kinase Degraders with In Vivo Activity. J Med Chem. 2023 Apr 13;66(7):4979-4998. |