HPK1-IN-7

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

HPK1-IN-7  纯度: 99.61%

HPK1-IN-7 是一种有效的口服活性 HPK1 (造血祖细胞激酶1, MAP4K1) 抑制剂(IC50=2.6 nM),具有优良的家族和激酶组选择性。HPK1-IN-7 对 IRAK4 (59 nM) 和 GLK (140 nM) 具有选择性。HPK1-IN-7 联合抗 PD1 对 MC38 同基因肿瘤模型显示出强大的疗效。

HPK1-IN-7

HPK1-IN-7 Chemical Structure

CAS No. : 2320462-65-3

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5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
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100 mg   询价  

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HPK1-IN-7 相关产品

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生物活性

HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1[1].

IC50 & Target[1]

HPK1

2.6 nM (IC50)

GLK/MAP4K3

140 nM (IC50)

IRAK4

59 nM (IC50)

Fms/CSFR

3.2 nM (IC50)

FLT3

25.4 nM (IC50)

AMPKA1

44.3 nM (IC50)

cKIT

45.7 nM (IC50)

MST1

55.1 nM (IC50)

ICK

65.1 nM (IC50)

MST2

78.5 nM (IC50)

体内研究
(In Vivo)

HPK1-IN-7 (100 mg/kg; p.o.; twice daily for 28 days) shows robust enhancement of anti-PD1 efficacy in a syngeneic tumor model of colorectal cancer[1].
HPK1-IN-7 (compound 24) (1 mg/kg; intravenous; mice) is characterized by moderate plasma clearance (43 mL/min/kg) and a large volume of distribution (4.4 L/kg). After oral administration (20 mg/kg), the Cmax was 5.3 μM and the AUC0-24h was 19 μM•h. The calculated oral bioavailability based on these pharmacokinetics studies is approximately 100%[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice (MC38 syngeneic tumor model)[1]
Dosage: 100 mg/kg
Administration: Oral; twice daily for 28 days
Result: Enhanced the efficacy of anti-PD1 treatment, garnering a 100% cure rate vs a 20% cure rate with anti-PD1 alone.

分子量

458.47

Formula

C24H22N6O4

CAS 号

2320462-65-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (272.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1812 mL 10.9058 mL 21.8117 mL
5 mM 0.4362 mL 2.1812 mL 4.3623 mL
10 mM 0.2181 mL 1.0906 mL 2.1812 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.54 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Degnan AP, et al. Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1. ACS Med Chem Lett. 2021;12(3):443-450. Published 2021 Feb 19.

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