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1630820-51-7

1630820-51-7 Structure

1630820-51-7 Structure
IdentificationBack Directory
[Name]

VNPP433-3β
[CAS]

1630820-51-7
[Synonyms]

VNPP433-3β
[Molecular Formula]

C29H34N4
[MOL File]

1630820-51-7.mol
[Molecular Weight]

438.61
Chemical PropertiesBack Directory
[Melting point ]

180-184 °C
[Boiling point ]

645.531±65.00 °C(Press: 760.00 Torr)(predicted)
[density ]

1.292±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
[form ]

Solid
[pka]

6.883±0.10(predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model[1].
[References]

[1] Thankan RS, et al., Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model. Bioorg Chem. 2023 Oct;139:106700. DOI:10.1016/j.bioorg.2023.106700
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