INCB086550 (PD-1/PD-L1-IN-8)是一种强效的口服小分子PD-L1抑制剂，IC50值为3.1nM。
Cas No.:2230911-59-6
Sample solution is provided at 25 µL, 10mM.
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INCB086550 (PD-1/PD-L1-IN-8) is a potent, oral, small-molecule PD-L1 inhibitor with an IC50 value of 3.1nM [1]. INCB086550 directly blocks the binding sites of PD-1 and PD-L1, and mediates the dimerization and endocytosis of PD-L1[2]. INCB086550 has been widely used in the humanized PD-L1 MC38 mouse model to inhibit tumor growth and for the pharmacodynamic comparison studies of different PD-L1 small molecule inhibitors[3].
In vitro, INCB086550 treatment (1μM) for 48 hours significantly inhibited the viability of CHO-K1 cells with overexpression of TCR activator and human PD-L1 on the cell surface[4]. Treatment with 1 µM INCB086550 for 18 hours blocked the PD-1-mediated signal transduction in CHO-K1 cells and stimulated cellular immune activation[5].
In vivo, INCB086550 treatment (15mg/kg; twice daily for 4 weeks) via intraperitoneal injection combined with Deucravacitinib reduced the tumor volume in 4T1-hPD-L1 cell-xenograft mouse models[6].
References:
[1] Yang D M, Kang Y W, Kim K, et al. Discovery of novel indoline derivatives as potent small molecule PD-L1 inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2025: 130458.
[2] Chen L, Zhao X, Liu X, et al. Development of small molecule drugs targeting immune checkpoints[J]. Cancer Biology & Medicine, 2024, 21(5): 382-399.
[3] Roose H, Rekstyte-Matiene K, Stevens S, et al. 1381 Discovery of ALG-093989, a highly potent and orally bioavailable small molecule PD-L1 inhibitor for the treatment of cancers[J]. 2023.
[4] Slota A, Golebiowska-Mendroch K, Kocik-Krol J, et al. Characterization of Clinically Evaluated Small-Molecule Inhibitors of PD-L1 for Immunotherapy[J]. ACS Medicinal Chemistry Letters, 2025.
[5] Koblish H K, Wu L, Wang L C S, et al. Characterization of INCB086550: a potent and novel small-molecule PD-L1 inhibitor[J]. Cancer Discovery, 2022, 12(6): 1482-1499.
[6] Xiang H, Tu B, Feng X, et al. Dual inhibition of TYK2 and PD-L1 boosts immune response in triple negative breast cancer[J]. Anti-Cancer Drugs, 2025, 36(4): 280-289.
INCB086550 (PD-1/PD-L1-IN-8)是一种强效的口服小分子PD-L1抑制剂，IC50值为3.1nM[1]。INCB086550直接阻断PD-1和PD-L1的结合位点，并介导PD-L1的二聚化和内吞作用[2]。INCB086550已被广泛用于人源化PD-L1 MC38小鼠模型，以抑制肿瘤生长，并用于不同PD-L1小分子抑制剂的药效比较研究[3]。
在体外，使用1µM的INCB086550处理48小时，显著抑制了细胞表面过表达TCR激活因子和人PD-L1的CHO-K1细胞的活力[4]。使用1µM的INCB086550处理18小时，阻断了CHO-K1细胞中PD-1介导的信号转导，并刺激了细胞免疫激活[6]。
在体内，每日两次腹腔注射INCB086550（15mg/kg），持续4周，联合Deucravacitinib治疗，减少了4T1-hPD-L1细胞异种移植小鼠模型中的肿瘤体积[6]。
| Cell experiment [1]: | |
Cell lines | CHO-K1 cells |
Preparation Method | CHO-K1 cells were cultured in F-12 medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). CHO-K1 cells were seeded at a density of 3×105 cells per well in a 6-well plate. After 24 hours, the cells were treated with different concentrations of INCB086550 (0.01, 0.1, 1, 10, 100, 1000, and 10000nM) for 18 hours. The cells were collected, washed with PBS, and stained with the fluorescently labeled anti-PD-L1 clone 28-8 at room temperature for 30 minutes. The samples were then analyzed using a flow cytometer. |
Reaction Conditions | 0.01, 0.1, 1, 10, 100, 1000, and 10000nM; 18h |
Applications | INCB086550 treatment decreased available surface PD-L1 in CHO-K1 in a dose of manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c mice |
Preparation Method | 6-week-old female BALB/c mice were housed under specific pathogen-free conditions with a 12-h light/dark cycle and provided with standard chow and water ad libitum. Mice were injected subcutaneously in the axilla with 5×106 4T1-hPD-L1 cells for each mouse. When the tumor volume in the mice reached approximately 100mm3 (around 1 week), mice were randomly assigned into four groups: the Vehicle group (Veh), the INCB086550 group (INC), the Deucravacitinib group (Deu), and the Combination group (Com). The Veh, INC, Deu, and Com groups were respectively intraperitoneally administered with the vehicle, 15mg/kg INCB086550 (twice daily), 20mg/kg Deucravacitinib (twice daily), and a combination of 15mg/kg INCB086550 (BID) plus 20mg/kg Deucravacitinib (twice daily). The vehicles for both Deucravacitinib and INCB086550 consisted of a solution with 5% dimethyl sulfoxide, 40% PEG300, 5% Tween 80, and 50% H2O. The administration of INCB086550 began 2 weeks prior to the initiation of Deucravacitinib treatment, with a total treatment duration of 4 weeks for INCB086550 and 2 weeks for Deucravacitinib. The mice were monitored twice weekly for body weight and tumor volume. |
Dosage form | 15mg/kg; twice daily for 4 weeks; i.p. |
Applications | INCB086550 treatment combined with Deucravacitinib reduced the tumor volume in 4T1-hPD-L1 cell-xenograft mouse models. |
References: | |
| Cas No. | 2230911-59-6 | SDF | |
| 别名 | PD-1/PD-L1-IN-8 | ||
| 分子式 | C41H39N7O4 | 分子量 | 693.79 |
| 溶解度 | H2O : 83.33 mg/mL (120.11 mM; ultrasonic and adjust pH to 3 with HCl) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4414 mL | 7.2068 mL | 14.4136 mL |
| 5 mM | 288.3 μL | 1.4414 mL | 2.8827 mL |
| 10 mM | 144.1 μL | 720.7 μL | 1.4414 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。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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