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2755761-78-3

2755761-78-3 Structure

2755761-78-3 Structure
IdentificationBack Directory
[Name]

(2S,4R)-1-[(2R)-2-[3-[(1S)-2-[(3R)-3-[(6aS)-5,6,6a,7,9,10-Hexahydro-2-(2-hydroxyphenyl)-8H-pyrazino[1′,2′:4,5]pyrazino[2,3-c]pyridazin-8-yl]-1-pyrrolidinyl]-1-methylethoxy]-5-isoxazolyl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-2-pyrrolidinecarboxamide
[CAS]

2755761-78-3
[Synonyms]

(2S,4R)-1-[(2R)-2-[3-[(1S)-2-[(3R)-3-[(6aS)-5,6,6a,7,9,10-Hexahydro-2-(2-hydroxyphenyl)-8H-pyrazino[1′,2′:4,5]pyrazino[2,3-c]pyridazin-8-yl]-1-pyrrolidinyl]-1-methylethoxy]-5-isoxazolyl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-2-pyrrolidinecarboxamide
[Molecular Formula]

C47H58N10O6S
[MOL File]

2755761-78-3.mol
[Molecular Weight]

891.09
Chemical PropertiesBack Directory
[density ]

1.40±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
[pka]

6.32±0.30(Predicted)
Hazard InformationBack Directory
[Uses]

PRT3789 is a SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 shows synergistic anti-proliferation effects with Adagrasib (HY-130149) in cancer cells. PRT3789 inhibits SMARCA4-mutated lung cancer proliferation. PRT3789 inhibits tumor growth in SMARCA4-deleted NSCLC models. Pink: SMARCA4 ligand (HY-44824) ; Blue: VHL ligand (HY-159465) ; Black: linker; VHL ligand+linker (HY-172738)[1].
[References]

[1] Koichi Ito, et al. Improved treatment of cancers using combinations of smarca2 degraders and kras targeting therapies. Patent. WO2024076985A2
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