2. MAPK/ERK Pathway
  3. MAP4K
  4. HPK1-IN-55

HPK1-IN-55 (compound 19) 是一种选择性且具有口服活性的造血祖细胞激酶 1 (HPK1) 抑制剂，其 IC50 为 <0.51 nM。 HPK1-IN-55 显示出优异的激酶选择性 (对 HPK1 的选择性高于 GCK 激酶和 LCK 的 637 倍和 1022 倍以上)。HPK1-IN-55 具有抗癌作用。

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HPK1-IN-55 Chemical Structure

HPK1-IN-55 Chemical Structure

CAS No. : 3048537-58-9

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HPK1-IN-55 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-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <0.51 nM. HPK1-IN-55 shows excellent kinase selectivity (>637-fold vs GCK-like kinase and >1022-fold vs LCK). HPK1-IN-55 has anticancer effects[1].

IC50 & Target[1]

HPK1

<0.51 nM (IC50)

体外研究
(In Vitro)

HPK1-IN-55 (0.5-10000 nM, 5 h) 在 human PBMCs 中显示出酶抑制作用 (IC50<0.51 nM) 和细胞效力 (EC50 = 43.3 nM) [1]。
HPK1-IN-55 (0.001-100 nM) 在 human PBMCs 中刺激 IL-2 和 IFN-γ 的释放，EC50 值分别为 38.8 和 49.2 nM[1]。
HPK1-IN-55 (0.00457-10 μM, 72 h) 在人体免疫 T 细胞中低、中、高浓度下均能促进 T 细胞增殖[1]。

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

HPK1-IN-55 相关抗体:

Cell Proliferation Assay [1]

Cell Line: human pan T cells
Concentration: 0.00457, 0.01372, 0.04115, 0.12346, 0.37037, 1.11111, 3.33333, 10 μM
Incubation Time: 72 h
Result: Increased T cell proliferation at low, intermediate and high concentrations in human pan T cells.
体内研究
(In Vivo)

HPK1-IN-55 (1.5-12 mg/kg, p.o., b.i.d, 5 weeks) 作为单一疗法具有良好的抗肿瘤作用，当与 anti-PD-1 联合使用时，在 CT26 模型中显示出相加作用，在 MC38 模型中表现出协同作用[1]。
HPK1-IN-55 (1 mg/kg, i.v., 2 mg/kg, p.o.) 在猴子体内表现出中等清除率 (Clp = 11.41 mL/min/kg)，良好的口服暴露 (DNAUC (0−24 h) =560.5 h•ng/mL) 和生物利用度 (F % = 42.0)[1]。
HPK1-IN-55 (1.5-12 mg/kg, p.o., b.i.d, 5 weeks) 在 CT26 模型中表现出良好的靶向参与[1]。
HPK1-In-55的体内药代动力学指标

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

HPK1-IN-55
beagle dogs IV Clp (mL/min/kg)
Vd (L/kg)		 11.44
5.58
beagle dogs PO DNAUC (0-24 h) (h・ng/ml)
t1/2 (h)
F (%)		 563
7.65
41.5
cyno monkeys IV Clp (mL/min/kg)
Vd (L/kg)		 11.41
5.07
cyno monkeys PO DNAUC (0-24 h) (h・ng/ml)
t1/2 (h)
F (%)		 560.5
8.73
42
Animal Model: Balb/c mice bearing the CT26 murine colorectal cancer tumor[1] .
Dosage: 3, 10, or 30 mg/kg
Administration: p.o., b.i.d, 24 h
Result: Animals receiving a 10 and 30 mg/kg dose exhibited a free plasma concentration that inhibited pSLP76 > 50% in the spleen for more than 6 h, whereas animals receiving the 3 mg/kg dose did not exhibit this sustained reduction.
Animal Model: Balb/c mice injected with CT26 cells[1] .
Dosage: 1.5, 12 mg/kg
Administration: p.o., b.i.d, 5weeks
Result: Exhibited a good antitumor response with a tumor growth inhibition (TGI) value of 64.3%.
Animal Model: Balb/c mice injected with MC38 cells[1] .
Dosage: 3, 12 mg/kg
Administration: p.o., b.i.d, 5weeks
Result: Demonstrated similar antitumor efficacy in the MC38 model with a TGI value of 34.9% for the 3 mg/kg group and 59.4% for the 12 mg/kg group.
分子量

554.64

Formula

C30H34N8O3
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-55 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-553048537-58-9MAP4KMAPK Kinase Kinase Kinaseantitumorhuman PBMCsimmunotherapyHPK1anticancer effectsInhibitorinhibitorinhibit

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目录号：
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