INCB086550
Based on 2 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.80%
- CAS 番号: 2230911-59-6
- 分子式: C41H39N7O4
- 分子量:693.79
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 INCB086550
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生物活性
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.
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Cell Line:Pleural effusion fluids cells
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Concentration:0.1-10000 nM
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Incubation Time:20 h
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Result:Had no overt toxicity to pleural effusion fluids cells.
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Cell Line:CHO PD-L1 cells
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Concentration:1 µmol/L
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Incubation Time:24 h
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Result:Decreased overall PD-L1 in CHO PD-L1 cells.
Demonstrated rapid internalization of PD-L1 that appeared maximal about 4 hours.
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.
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Animal Model:mice bearing MDA-MB-231 xenografts[1]
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Dosage:15, 200 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Reduced unoccupied cell-surface PD-L1 on MDA-MB-231 tumors at 24 hours.
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Animal Model:C57BL/6 and NSG mice bearing established MC38-huPD-L1 tumors[1]
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Dosage:2, 20, or 200 mg/kg
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Administration:Oral gavage (p.o.)
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2230911-59-6
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性状 Solid
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分子量 693.79
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分子式 C41H39N7O4
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Color Light yellow to yellow
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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
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別名
PD-1/PD-L1-IN-8
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
2026 Mar 7:117871. PMID: 41802682 -
Anticancer Drugs
Dual inhibition of TYK2 and PD-L1 boosts immune response in triple negative breast cancer. [Abstract]2025 Apr 1;36(4):280-289. PMID: 39774369
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
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.
INCB086550 関連分類
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