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ChemicalBook--->CAS DataBase List--->2447066-37-5

2447066-37-5

2447066-37-5 Structure

2447066-37-5 Structure
IdentificationBack Directory
[Name]

INDEX NAME NOT YET ASSIGNED
[CAS]

2447066-37-5
[Synonyms]

PROTAC PD-1/PD-L1 degrader-1
[Molecular Formula]

C59H58ClN7O11
[MOL File]

2447066-37-5.mol
[Molecular Weight]

1076.6
Chemical PropertiesBack Directory
[density ]

1.45±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C, sealed storage, away from moisture and light
[solubility ]

DMSO : 210 mg/mL (195.06 mM; Need ultrasonic)
[form ]

Solid
[pka]

10.69±0.40(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner[1].
[Biological Activity]

PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner[1]. PROTAC PD-1/PD-L1 degrader-1 (compound p22) reduces cell surface PD-L1 expression for more than 14%[1].PROTAC PD-1/PD-L1 degrader-1 (1-10 μM; 24 hours) reduces PD-L1 expression in a dose-dependent manner by 21% and 35% at 1 μM and 10 μM, respectively[1].
[IC 50]

Cereblon
[References]

[1]. Cheng B, Ren Y, Cao H, Chen J. Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1. Eur J Med Chem. 2020;199:112377.
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