GLPBio

INCB086550 (PD-1/PD-L1-IN-8)

Catalog No.: GC62688Purity:>98.00%Synonyms: PD-1/PD-L1-IN-8
COASDSData Sheet
PD-1/PD-L1-IN-8 (PD-1/PD-L1-IN-8; Beispiel 24) ist ein PD-1/PD-L1-Inhibitor mit einem IC50 <= 10 nM.

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INCB086550 (PD-1/PD-L1-IN-8)
Cas No.: 2230911-59-6
1mgIn Stock
$106.00
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5mgIn Stock
$224.00
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10mgIn Stock
$326.00
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

Beschreibung (Description)

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.

Protokoll (Protocol)

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:
[1] 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.
[2] 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.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
2230911-59-6
Synonyme
PD-1/PD-L1-IN-8
Summenformel
C41H39N7O4
Molekulargewicht
693.79
Löslichkeit
H2O : 83.33 mg/mL (120.11 mM; ultrasonic and adjust pH to 3 with HCl)
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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