| Identification | Back Directory | [Name]
3-Pyrrolidinecarboxylic acid, 1-[[7-cyano-2-[3'-[[3-[[(3R)-3-hydroxy-1-pyrrolidinyl]methyl]-1,7-naphthyridin-8-yl]amino]-2,2'-dimethyl[1,1'-biphenyl]-3-yl]-5-benzoxazolyl]methyl]-, (3R)- | [CAS]
2230911-59-6 | [Synonyms]
INCB084550
PD-1/PD-L1-IN-8
3-Pyrrolidinecarboxylic acid, 1-[[7-cyano-2-[3'-[[3-[[(3R)-3-hydroxy-1-pyrrolidinyl]methyl]-1,7-naphthyridin-8-yl]amino]-2,2'-dimethyl[1,1'-biphenyl]-3-yl]-5-benzoxazolyl]methyl]-, (3R)-
3-Pyrrolidinecarboxylic acid, 1-[[7-cyano-2-[3'-[[3-[[(3R)-3-hydroxy-1-pyrrolidinyl]methyl]-1,7-naphthyridin-8-yl]amino]-2,2'-dimethyl[1,1'-biphenyl]-3-yl]-5-benzoxazolyl]methyl]-, (3R)- ISO 9001：2015 REACH | [Molecular Formula]
C41H39N7O4 | [MDL Number]
MFCD34549780 | [MOL File]
2230911-59-6.mol | [Molecular Weight]
693.79 |
| Chemical Properties | Back Directory | [Boiling point ]
859.8±65.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Ethanol: Soluble
Methanol: Soluble
Water: Soluble | [form ]
Solid | [pka]
14.75±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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 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].
| 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.
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| [References]
[1] WU LIANGXING, et al. BENZOOXAZOLE DERIVATIVES AS IMMUNOMODULATORS. WO2018119266A1.
[2] Koblish HK, et al. Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor. Cancer Discov. 2022 Jun 2;12(6):1482-1499. DOI:10.1158/2159-8290.CD-21-1156 |
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| Company Name: |
Twochem Co.Ltd
|
| Tel: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
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