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)- Basic information
- Product 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)-
- Synonyms:
-
- 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)-
- INCB084550
- 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
- PD-1/PD-L1-IN-8
- (R)-1-((7-Cyano-2-(3'-((3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-yl)amino)-2,2'-dimethyl-[1,1'-biphenyl]-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid
- INCB086550(INCB-086550)
- INCB086550 ，S9863
- CAS:
- 2230911-59-6
- MF:
- C41H39N7O4
- MW:
- 693.79
- Product Categories:
-
- API
- Mol File:
- 2230911-59-6.mol
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)- Chemical Properties
- 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
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)- Usage And Synthesis
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. |
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
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)-Supplier
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