PD-1/PD-L1-IN-9

目录号: GC62387纯度: >99.50%

PD-1/PD-L1-IN-9是一种强效且口服有效的PD-1/PD-L1抑制剂，IC₅₀值为3.8nM。

Cas No.: 2628506-54-5

规格	价格	库存	数量
1mg	¥556.00	现货	1
5 mg	¥1,390.00	现货	1
10 mg	¥1,980.00	现货	1
25 mg	¥3,330.00	现货	1
50mg	¥4,530.00	现货	1
100mg	¥5,920.00	现货	1
200mg	¥7,930.00	现货	1
10mM (in 1mL DMSO)	¥1,090.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1, with an IC₅₀ value of 3.8nM^[1]. The aminoethanol tail of PD-1/PD-L1-IN-9 interacts with AAsp122 and BGln66 via two hydrogen bonds and contributes to the high binding affinity to dimeric PD-L1^[¹^]. PD-1/PD-L1-IN-9 has been widely used to block inhibition of PD-1 reporter T cells^[²^].

In vivo, PD-1/PD-L1-IN-9 treatment via oral administration at a dose of 80mg/kg/day for 2 weeks significantly inhibited tumor growth in the CT26 mouse model^[1].

References:
[1] Wang T, Cai S, Wang M, et al. Novel biphenyl pyridines as potent small-molecule inhibitors targeting the programmed cell death-1/programmed cell death-ligand 1 interaction[J]. Journal of Medicinal Chemistry, 2021, 64(11): 7390-7403.
[2] Leitner J, Schindler H, Gumpelmair S, et al. Evaluation of small molecule PD-1/PD-L1 inhibitors in a T cell reporter system[J]. Biochemical Pharmacology, 2026: 117871.

PD-1/PD-L1-IN-9是一种强效且口服有效的PD-1/PD-L1抑制剂，IC₅₀值为3.8nM^[1]。PD-1/PD-L1-IN-9的氨基乙醇尾部通过两个氢键与Asp122和Gln66相互作用，有助于与二聚体PD-L1的高结合亲和力^[1]。PD-1/PD-L1-IN-9 已被广泛用于阻断 PD-1 报告T细胞的抑制作用^[2]。

在体内，口服给予80mg/kg/day剂量的PD-1/PD-L1-IN-9治疗2周，显著抑制了CT26小鼠模型中的肿瘤生长^[1]。

实验参考方法 Experimental Reference Method

Animal experiment [1]:
Animal models	BALB/c mice
Preparation Method	Male BALB/c mice between 5 and 6 weeks in age were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility with food and tap water ad libitum. A total of 5×10⁵ CT26 cells were inoculated into the right flank of each mouse. Mice in control groups were treated with 200μl of vehicle solution only. Mice were treated with vehicle control and PD-1/PD-L1-IN-9 (80mg/kg) by intragastric gavage once a day for 2 weeks. The tumor volume sizes were measured every 2 days with a caliper and calculated with the formula 0.5×length×width.
Dosage form	80mg/kg/day for 2 weeks; p.o.
Applications	PD-1/PD-L1-IN-9 treatment significantly inhibited tumor growth in the CT26 mouse model.
References: [1] Wang T, Cai S, Wang M, et al. Novel biphenyl pyridines as potent small-molecule inhibitors targeting the programmed cell death-1/programmed cell death-ligand 1 interaction[J]. Journal of Medicinal Chemistry, 2021, 64(11): 7390-7403.

产品文档 Product Documents

批次：Purity:>99.50%

化学性质Chemical Properties

CAS 号

2628506-54-5

分子式

C₂₂H₂₄N₂O₂

分子量

348.44 g/mol

溶解性

DMSO : 100 mg/mL (286.99 mM; Need ultrasonic)

保存条件

Store at -20°C

General tips

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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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