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Galeterone

CAT: 0804-HY-70006-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-70006-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
CYP17

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