2. MAPK/ERK Pathway
  3. MAP4K
  4. HPK1-IN-62

HPK1-IN-62 是一种有选择性和口服活性的 HPK-1 抑制剂，其 IC50 为 1.22 nM。HPK1-IN-62 显著提高了 GLK 选择性 (> 665 倍) 和 LCK 选择性 (> 1095 倍)。HPK1-IN-62 可增强 T 细胞活化，并在 MC38 肿瘤模型中与抗 mPD-1 疗法联合使用时表现出协同作用，从而抑制肿瘤生长。HPK1-IN-62 可用于结肠癌和癌症免疫的研究。

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HPK1-IN-62

HPK1-IN-62 Chemical Structure

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HPK1-IN-62 相关抗体

Top Publications Citing Use of Products

查看 MAP4K 亚型特异性产品:

查看所有亚型
MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HPK1-IN-62 is a selective and orally active HPK-1 inhibitor with an IC50 of 1.22 nM. HPK1-IN-62 significantly improves GLK selectivity (> 665-fold) and LCK selectivity (> 1095-fold). HPK1-IN-62 enhances T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1 therapy in the MC38 tumor model, inhibiting a tumor growth. HPK1-IN-62 can be used in the researchs of colon cancer and cancer immunotherapy[1].

IC50 & Target[1]

HPK1

1.22 nM (IC50)

GLK/MAP4K3

812 nM (IC50)

GCK/MAP4K2

1336.9 nM (IC50)

体外研究
(In Vitro)

HPK1-IN-62 (Compound 2t) (0-10 μM ,5.2 h) 可有效抑制外周血单核细胞 (PBMC) 中 SLP76 的磷酸化，IC50 为 1.7 μM[1]。
HPK1-IN-62 (1 μM) 在人肝微粒体中表现出优异的代谢稳定性[1]。

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

HPK1-IN-62 相关抗体:
体内研究
(In Vivo)

HPK1-IN-62 (Compound 2t) (100 mg/kg，口服，每日两次，持续 14 天) 在 MC38 小鼠模型中与 mPD-1 抗体表现出协同作用[1]。

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

Animal Model: MC38 cells xenograft model established in female C57BL/6 mice, aged 6-7 weeks[1]
Dosage: 100 mg/kg with or without anti-mPD-1
Administration: Oral administration (p.o.), twice daily for 14 days
Result: Did not show significant tumor-suppressive effects as monotherapy.
Enhanced T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1, achieving a tumor growth inhibition (TGI) rate of 76%, compared to 70% with anti-mPD-1 monotherapy.
分子量

563.65

Formula

C32H33N7O3
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

HPK1-IN-62 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:

HPK1-IN-62MAP4KMAPK Kinase Kinase KinaseCancer immunotherapyHPK1 kinase inhibitorMacrocyclizationPyridineSelectivityInhibitorinhibitorinhibit

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产品名称：
HPK1-IN-62
目录号：
HY-178097
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