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

ITK degrader 1 是一种高度选择性的白细胞介素 2 诱导的 T 细胞激酶 (ITK) 降解剂 (DC50=3.6 nM)。ITK degrader 1 快速、持久地诱导 ITK 降解，并抑制体内抗 CD3 抗体刺激的 IL-2 分泌 (EC50=35.2 nM，Jurkat 细胞)。ITK degrader 1 也显示出良好的血浆暴露水平。

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ITK degrader 1 Chemical Structure

ITK degrader 1 Chemical Structure

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ITK degrader 1 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ITK degrader 1 相关抗体:

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.
体内研究
(In Vivo)

ITK degrader 1 (compound 28) (20 mg/kg；腹腔注射；单剂量) 处理小鼠 2 小时、8 小时和 16 小时后，显著降解 ITK 蛋白[1]。ITK degrader 1 (25 mg/kg；腹腔注射；单剂量) 在抗 CD3 单克隆抗体 (mAb) 诱导的 IL-2 小鼠模型中，处理 6 小时后抑制 IL-2 分泌[1]。


在 Balb/c 小鼠中的药代动力学分析[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%

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.
分子量

943.02

Formula

C48H57F3N10O7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ITK degrader 1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-1ItkPROTACsInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseInhibitorinhibitorinhibit

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