Galeterone

Galeterone (TOK-001) is a potent, 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. Galeterone also functions as a CYP17 inhibitor (IC50 = 47 nM) . Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].

Product Specifications

CAS Number

[851983-85-2]

Product Name Alternative

TOK-001; VN-124-1

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Androgen Receptor; Apoptosis; Cytochrome P450; MNK; Molecular Glues

Type

Reference compound

Related Pathways

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

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TOK-001.html

Purity

99.87

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

C[C@@]12C(N3C=NC4=CC=CC=C34)=CC[C@]1([C@@]5(CC=C6[C@@](C)([C@]5(CC2)[H])CC[C@@H](C6)O)[H])[H]

Molecular Formula

C26H32N2O

Molecular Weight

388.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Bruno RD, et al. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001) : head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.Steroid|[2]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.