2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. INCB086550

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

Cat. No.: HY-134884 Purity: 99.80%
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INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research.

For research use only. We do not sell to patients.

INCB086550 Chemical Structure

INCB086550 Chemical Structure

CAS No. : 2230911-59-6

Size Price Stock Quantity
1 mg USD 135 In-stock
5 mg USD 460 In-stock
10 mg USD 735 In-stock
25 mg USD 1180 In-stock
50 mg USD 1652 In-stock
100 mg USD 2400 In-stock
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Based on 1 publication(s) in Google Scholar

INCB086550 Related Antibodies

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Description

INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research[1].

In Vitro

INCB086550 (0.1-10000 nM, 20 h) has no overt toxicity to pleural effusion fluids cells[1].
INCB086550 (1 µmol/L, 24 h) induces the dimerization of cell-surface PD-L1 and resulting in internalization[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

INCB086550 Related Antibodies

Cell Viability Assay [1]

Cell Line: Pleural effusion fluids cells
Concentration: 0.1-10000 nM
Incubation Time: 20 h
Result: Had no overt toxicity to pleural effusion fluids cells.

Immunofluorescence [1]

Cell Line: CHO PD-L1 cells
Concentration: 1 µmol/L
Incubation Time: 24 h
Result: Decreased overall PD-L1 in CHO PD-L1 cells.
Demonstrated rapid internalization of PD-L1 that appeared maximal about 4 hours.
In Vivo

INCB086550 (15, 200 mg/kg for Oral gavage, once or twice) inhibits greater than 90% of unoccupied cell surface PD-L1 in MDA-MB-231 mice model[1].
INCB086550 (2, 20, or 200 mg/kg for Oral gavage, b.i.d) inhibits tumor growth in MC38 huPD-L1 mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: mice bearing MDA-MB-231 xenografts[1]
Dosage: 15, 200 mg/kg
Administration: Oral gavage (p.o.)
Result: Reduced unoccupied cell-surface PD-L1 on MDA-MB-231 tumors at 24 hours.
Animal Model: C57BL/6 and NSG mice bearing established MC38-huPD-L1 tumors[1]
Dosage: 2, 20, or 200 mg/kg
Administration: Oral gavage (p.o.)
Result: Induced a dose-dependent decrease of PD-L1 available to bind to PD-1 using antibody clone MIH1.
Reduced occupied cell-surface PD-L1 > 90% at the 200 mg/kg dose.
Clinical Trial
Molecular Weight

693.79

Formula

C41H39N7O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=C2C(N=C(C3=C(C(C4=C(C(NC5=NC=CC6=C5N=CC(CN7CC[C@H](C7)O)=C6)=CC=C4)C)=CC=C3)C)O2)=CC(CN8C[C@@H](CC8)C(O)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (144.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 83.33 mg/mL (120.11 mM; ultrasonic and adjust pH to 3 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4414 mL 7.2068 mL 14.4136 mL
5 mM 0.2883 mL 1.4414 mL 2.8827 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.80%

COA (246 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.4414 mL 7.2068 mL 14.4136 mL 36.0340 mL
5 mM 0.2883 mL 1.4414 mL 2.8827 mL 7.2068 mL
10 mM 0.1441 mL 0.7207 mL 1.4414 mL 3.6034 mL
15 mM 0.0961 mL 0.4805 mL 0.9609 mL 2.4023 mL
20 mM 0.0721 mL 0.3603 mL 0.7207 mL 1.8017 mL
25 mM 0.0577 mL 0.2883 mL 0.5765 mL 1.4414 mL
30 mM 0.0480 mL 0.2402 mL 0.4805 mL 1.2011 mL
40 mM 0.0360 mL 0.1802 mL 0.3603 mL 0.9008 mL
50 mM 0.0288 mL 0.1441 mL 0.2883 mL 0.7207 mL
60 mM 0.0240 mL 0.1201 mL 0.2402 mL 0.6006 mL
80 mM 0.0180 mL 0.0901 mL 0.1802 mL 0.4504 mL
100 mM 0.0144 mL 0.0721 mL 0.1441 mL 0.3603 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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INCB086550 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

INCB0865502230911-59-6PD-1/PD-L1-IN-8INCB 086550INCB-086550PD-1/PD-L1PD-1/Programmed death-ligand 1PD-L1antitumorimmunesmall-moleculeInhibitorinhibitorinhibit

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