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INCB086550
CAS No. 2230911-59-6
INCB086550( —— )
Catalog No. M34893 CAS No. 2230911-59-6
INCB086550 (PD-1/PD-L1-IN-8) (example 24) is a PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 359 | In Stock |
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| 10MG | 540 | In Stock |
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| 25MG | 867 | In Stock |
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| 50MG | 1144 | In Stock |
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| 100MG | 1562 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameINCB086550
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NoteResearch use only, not for human use.
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Brief DescriptionINCB086550 (PD-1/PD-L1-IN-8) (example 24) is a PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM.
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DescriptionINCB086550 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.
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In VitroCell Viability Assay 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 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.
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In VivoAnimal Model:mice bearing MDA-MB-231 xenografts 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 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.
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Synonyms——
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PathwayImmunology/Inflammation
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TargetPD-1/PD-L1
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RecptorPD-1/PD-L1
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Research Area——
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Indication——
Chemical Information
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CAS Number2230911-59-6
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Formula Weight693.79
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Molecular FormulaC41H39N7O4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?H2O : 83.33 mg/mL (120.11 mM; Ultrasonic; (HCL ，pH≈3))
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SMILESCc1c(Nc2nccc3cc(CN4CC[C@@H](O)C4)cnc23)cccc1-c1cccc(-c2nc3cc(CN4CC[C@H](C4)C(O)=O)cc(C#N)c3o2)c1C
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. WU LIANGXING, et al. BENZOOXAZOLE DERIVATIVES AS IMMUNOMODULATORS. WO2018119266A1.
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