2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. E1/E2/E3 Enzyme Interleukin Related
  4. Cbl-b-IN-29

Cbl-b-IN-29 是一种口服有效的 CBL-B 抑制剂。CBL-B 结合活性口袋从而有效抑制免疫 E3 泛素连接酶的功能。Cbl-b-IN-29 可以诱导 Jurkat 细胞释放 IL-2 (EC50 = 159 nM)。Cbl-b-IN-29 在体内表现出强大的抗肿瘤功效，且具有良好的耐受性，未观察到不良反应。Cbl-b-IN-29 可用于癌症免疫，结肠癌和肿瘤免疫联合的相关研究。

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Cbl-b-IN-29

Cbl-b-IN-29 Chemical Structure

CAS No. : 3070411-10-5

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Cbl-b-IN-29 相关抗体

Top Publications Citing Use of Products

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cbl-b-IN-29 is an orally active CBL-B inhibitor. Cbl-b-IN-29 binds to the CBL-B active pocket. Cbl-b-IN-29 induces Jurkat cell release IL-2 with an EC50 of 159 nM, effectively inhibiting the function of immune E3 ubiquitin ligase. Cbl-b-IN-29 demonstrates robust anti-tumor efficacy in vivo with good tolerability and no observed adverse reactions. Cbl-b-IN-29 can be used for cancer immunotherapy, colorectal cancer and immune-oncology combination research[1].

体外研究
(In Vitro)

Cbl-b-IN-29 (compound 20) 具有较低的 CYP 抑制/诱导风险及 hERG 抑制风险[1]。

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

Cbl-b-IN-29 相关抗体:
体内研究
(In Vivo)

Cbl-b-IN-29 (compound 20) (30 mg/kg，口服，每日一次共计 15 天) 在鼠源 CT26 同源肿瘤小鼠模型中，无论是作为单一疗法还是与 anti-mouse PD-1 抗体联合使用，均表现出良好的抗肿瘤功效和动物耐受性，且未观察到不良反应[1]。

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

Animal Model: CT26 tumor cells (3×105)-induced BALB/c mice (6-8 weeks)[1]
Dosage: 30 mg/kg
Administration: p.o., once daily for 15 days
Result: Resulted in a robust anti-tumor efficacy with a tumor growth inhibition (TGI) of 76%.
Indicated a low risk for CYP inhibition/induction and herg inhibition.
Exhibited good animal tolerability, with no observed adverse 412 reactions. .
分子量

499.62

Formula

C30H34FN5O
CAS 号
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

Cbl-b-IN-29 相关分类

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  • 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:

Cbl-b-IN-293070411-10-5E1/E2/E3 EnzymeInterleukin RelatedE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseILimmune E3 ubiquitin ligaseimmunotherapyimmune-oncology combinationCBL-BInhibitorinhibitorinhibit

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