VNPP433-3β

VNPP433-3β (Galeterone 3β-imidazole) is an orally active 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 induces cell apoptosis. VNPP433-3β inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) [1].

Product Specifications

CAS Number

[1630820-51-7]

Product Name Alternative

Galeterone 3β-imidazole

UNSPSC

12352005

Target

Androgen Receptor; Apoptosis; MNK; Molecular Glues

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway; PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vnpp433-3β.html

Purity

98.01

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C[C@@]12[C@](CC=C2N3C4=CC=CC=C4N=C3)([H])[C@@]5([H])[C@]([C@@]6(C(C[C@@H](N7C=CN=C7)CC6)=CC5)C)([H])CC1

Molecular Formula

C29H34N4

Molecular Weight

438.61

References & Citations

[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.