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
Sample solution is provided at 25 µL, 10mM.
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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]。
| 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: | |
| Cas No. | 2628506-54-5 | SDF | |
| 分子式 | C22H24N2O2 | 分子量 | 348.44 |
| 溶解度 | DMSO : 100 mg/mL (286.99 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8699 mL | 14.3497 mL | 28.6993 mL |
| 5 mM | 574 μL | 2.8699 mL | 5.7399 mL |
| 10 mM | 287 μL | 1.435 mL | 2.8699 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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- Purity: >99.50% Appearance: A solid
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