ChemicalBook > CAS DataBase List > 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)-

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)-
CAS No.: 2230911-59-6
Chemical 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: INCB084550;PD-1/PD-L1-IN-8;INCB086550 ，S9863;INCB086550(INCB-086550);(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;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
CBNumber: CB68225607
Molecular Formula: C41H39N7O4
Formula Weight: 693.79
MOL File: 2230911-59-6.mol

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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)- Property

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

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Hazard and Precautionary Statements (GHS)

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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,Usage,Production

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)- Preparation Products And Raw materials

Raw materials

Preparation Products

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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)- Suppliers

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2230911-59-6, 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)-Related Search:

INCB39110 INCB-54329

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

2230911-59-6

C41H39N7O4

API