HPK1-IN-7|cas:2320462-65-3|西域试剂

HPK1-IN-7,99.61%

产品编号：Bellancom-138742| CAS NO：2320462-65-3| 分子式：C₂₄H₂₂N₆O₄| 分子量：458.47

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货号	价格	库存与货期
Bellancom-138742	￥3500.00	杭州北京（现货）
Bellancom-138742	￥5800.00	杭州北京（现货）
Bellancom-138742	￥11000.00	杭州北京（现货）

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HPK1-IN-7

产品介绍

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。

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.

体外研究

体内研究

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.
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 AUC_0-24h was 19 μM•h. The calculated oral bioavailability based on these pharmacokinetics studies is approximately 100%.

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

Animal Model:	Mice (MC38 syngeneic tumor model)
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.

体内研究

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

Animal Model:	Mice (MC38 syngeneic tumor model)
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.

性状

Solid

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