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2374856-75-2

2374856-75-2 Structure

2374856-75-2 Structure
IdentificationBack Directory
[Name]

(5S,5'S)-5,5'-((((5,5'-(2,2'-dichloro-[1,1'-biphenyl]-3,3'-diyl)bis(3-methoxypyrazine-5,2-diyl))bis(methylene))bis(azanediyl))bis(methylene))bis(pyrrolidin-2-one)
[CAS]

2374856-75-2
[Synonyms]

Evixapodlin
PD-1/PD-L1-IN 7
(5S,5'S)-5,5'-((((5,5'-(2,2'-DICHLORO-[1,1'-BIPHENYL]-3,3'-DIYL)BIS(3-METHOXYPYRAZINE-5,2-DIYL))BIS(
2-Pyrrolidinone, 5,5'-[(2,2'-dichloro[1,1'-biphenyl]-3,3'-diyl)bis[(3-methoxy-5,2-pyrazinediyl)methyleneiminomethylene]]bis-, (5S,5'S)-
(5S,5'S)-5,5'-((((5,5'-(2,2'-dichloro-[1,1'-biphenyl]-3,3'-diyl)bis(3-methoxypyrazine-5,2-diyl))bis(methylene))bis(azanediyl))bis(methylene))bis(pyrrolidin-2-one)
[Molecular Formula]

C34H36Cl2N8O4
[MOL File]

2374856-75-2.mol
[Molecular Weight]

691.61
Chemical PropertiesBack Directory
[Boiling point ]

817.1±65.0 °C(Predicted)
[density ]

1.310±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 50 mg/mL (72.30 mM; Need ultrasonic)
[form ]

Solid
[pka]

15.81±0.40(Predicted)
[color ]

White to yellow
Hazard InformationBack Directory
[Uses]

Evixapodlin (GS-4224) is a human PD-1/PD-L1 protein/protein interaction inhibitor with an IC50 of 0.213 nM. Evixapodlin has anticancer and antiviral functions[1].
[in vivo]

Evixapodlin (Compound 139; 10-50 mg/kg; intraperitoneal injection, daily, for 6 days) treatment shows >90% PD-L1 target occupancy (TO) on the tumor cells. Evixapodlin significantly inhibits tumor growth in a human PD-L1 expressing MC38 mouse colorectal tumor model[1].

Animal Model:Female C57BL/6 mice injected with MC38 tumor cells[1]
Dosage:10 mg/kg, 25 mg/kg, and 50 mg/kg
Administration:Intraperitoneal injection, daily, for 6 days
Result:Showed greater than 90% TO on the tumors and inhibited tumor growth in vivo.
[References]

[1] Evangelos Aktoudianakis, et al. Pd-1/pd-l1 inhibitors. WO2019160882A1.
Spectrum DetailBack Directory
[Spectrum Detail]

(5S,5'S)-5,5'-((((5,5'-(2,2'-dichloro-[1,1'-biphenyl]-3,3'-diyl)bis(3-methoxypyrazine-5,2-diyl))bis(methylene))bis(azanediyl))bis(methylene))bis(pyrrolidin-2-one)(2374856-75-2)1HNMR
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