2. MAPK/ERK Pathway
  3. MAP4K
  4. HPK1-IN-40-d2

HPK1-IN-40 是高效、高选择性的 HPK1 抑制剂，IC50 为 0.9 nM。HPK1-IN-40 激活 T 细胞受体 (TCR) 信号，促进 T 细胞功能与细胞因子的产生且具有抗癌活性。

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HPK1-IN-40-d<sub>2</sub> Chemical Structure

HPK1-IN-40-d2 Chemical Structure

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3.  试用装只面向终端客户。

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Customer Review

HPK1-IN-40-d2 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-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity[1].

IC50 & Target

HPK1[1]IC50: 0.9 nM[1]
体外研究
(In Vitro)

HPK1-IN-40 (0.1 μM, 1 μM) 促进Jurkat细胞的IL-2分泌且抑制T细胞中的HPK1信号转导，进而增强T细胞功能[1]。
HPK1-IN-40 (0.03 μM ~ 1 μM ) 抑制T细胞中HPK1信号通路[1]。
1.19
HPK1-IN-40在大鼠体内的药动学参数[1]

Route Parameter Rat (1 mg/kg)
IV T1/2(h) 0.898
AUClast(h*ng/mL) 355
Vss(L/kg) 2.45
Clhep (mL/min/kg) 46.8
Route Parameter Rat (3 mg/kg)
PO T1/2 (h) 0.499
Tmax (h) 0.250
AUClast(h*ng/mL) 1.91
Cmax (ng/mL) 3.62
F% 0.179

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

HPK1-IN-40-d2 相关抗体:

Western Blot Analysis[1]

Cell Line: Jurkat, primary mouse T cells
Concentration: 0.03, 0.1, 0.3, 1 (μM)
Incubation Time: 1h
Result: Inhibited the HPK1 signaling in T cells.
体内研究
(In Vivo)

HPK1-IN-40单独 (25 mg/kg; i.p.; bid for 7 days) 导致CT26荷瘤小鼠体内T细胞激活，产生免疫调节[1]。
HPK1-IN-40 (25 mg/kg; i.p.; bid for 10 days) 联合抗PD1抗体 (10 mg/kg; i.p.; bid for 10 days) 表现出协同抗肿瘤作用，HPK1-IN-40联合抗pd1抗体组CT26肿瘤生长幅度最低，没有观察到明显的体重减轻，表明治疗耐受性良好[1]。

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

Animal Model: CT26 Tumor-bearing mice
Dosage: 25 mg/kg
Administration: Twice a day by intraperitoneal injection (i.p.), bid for 7 days.
Result: Increased IFN-γ+CD3+ T in CD3+ TIL, IFN-γ+CD8+ T in CD8+ TIL, Th1 in CD4+ TIL, CD69+CD3+ T in CD3+ TIL, CD69+CD8+ T in CD8+ TIL, CD69+CD4+ T in CD4+ TIL.
Animal Model: CT26 Tumor-bearing mice
Dosage: HPK1-IN-40 (25 mg/kg), anti-PD1 antibody (10 mg/kg)
Administration: HPK1-IN-40 alone / anti-PD1 antibody alone (every 3 days), or the combination treatment, twice a day by intraperitoneal injection (i.p.) for 10 days.
Result: Showed marginal tumor growth inhibition (TGI = 19.6%). The CT26 tumor growth rate of HPK1-IN-40 combined with anti-PD1 antibody was the lowest, then anti-PD1 alone, then HPK1-IN-40. No significant body weight loss was observed.
分子量

477.49

Formula

C24H20D2FN7O3
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.
溶解性数据

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

  • 方案 一

    Dissolved in 2.5% DMSO, 5% HS 15, 22.5% poly(ethylene glycol) 400, and 70% physiological saline.

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

HPK1-IN-40-d2 相关分类

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-40-d2MAP4KMAPK Kinase Kinase KinaseJurkat cellsCT-26colon tumor modelcancerTMEHPK1Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-149773S
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