2. MAPK/ERK Pathway
  3. MAP4K
  4. HPK1-IN-52

HPK1-IN-52 是一种有效的具有口服活性的造血祖细胞激酶 1 (HPK1) 抑制剂，IC50 值为 10.4 nM。HPK1-IN-52 表现出抗肿瘤活性。

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HPK1-IN-52 Chemical Structure

HPK1-IN-52 Chemical Structure

CAS No. : 2994298-66-5

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HPK1-IN-52 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-52 is a potent and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 10.4 nM. HPK1-IN-52 exhibits anti-tumor activities[1].

IC50 & Target[1]

HPK1

10.4 nM (IC50)

MAP4K2

448 nM (IC50)

GLK/MAP4K3

85 nM (IC50)

MAP4K4

665 nM (IC50)

MAP4K5

104 nM (IC50)

MAP4K6

168 nM (IC50)

体外研究
(In Vitro)

HPK1-IN-52 (compound 24) 表现出相当的活性（IC50 为 10.4 nM）和细胞效力（pSLP76 EC50 为 41 nM 和 IL-2 EC50 为 108 nM）[1]。

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

HPK1-IN-52 相关抗体:
体内研究
(In Vivo)

HPK1-IN-52（compound 24；30 mg/kg；口服；每日两次；持续两周）表现出中等程度的肿瘤生长抑制 (TGI)，为 42%[1]。
HPK1-IN-52 在小鼠中的血浆清除率显著提高 (Clp = 46 mL/min/kg)，其口服暴露量显著增加 (AUC(0–24h) = 4139 h ng/mL)。此外，HPK1-IN-52 在大鼠中表现出较低的体内清除率 (Clp = 67 mL/min/kg) 和较高的口服暴露量 (AUC(0–24h) = 2013 h ng/mL)[1]。

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

Animal Model: Balb/c mice injected with CT26 cells[1]
Dosage: 30 mg/kg
Administration: po; twice daily; for two weeks
Result: Exhibited moderate tumor-growth inhibition.
分子量

556.61

Formula

C31H30F2N6O2
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

HPK1-IN-52 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-522994298-66-5MAP4KMAPK Kinase Kinase KinaseHPK1 inhibitororally activeanti-tumor activitiesInhibitorinhibitorinhibit

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产品名称：
HPK1-IN-52
目录号：
HY-168110
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