Galeterone hydrochloride
Based on 3 publication(s) in Google Scholar
Galeterone (TOK-001) hydrochloride 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 hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].
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- CAS No.: 1239339-17-3
- Formule: C26H33ClN2O
- Masse moléculaire:425.01
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Galeterone hydrochloride
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Activité biologique
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CYP17 47 nM (IC50) |
MNK1 |
MNK2 |
Galeterone hydrochloride (compound 3) possess potent antiproliferative activities with GI50 of 0.36 μM, 0.21 μM, 0.56 μM against LNCaP (androgen-sensitive), C42B (androgen-insensitive) and CWR22Rv1 (castration-resistant), respectively[1].
Galeterone hydrochloride (5-20 μM; 24 h) can degrade AR/AR-V7 and Mnk1/2 with consequent inhibition of AR signaling and depletion of peIF4E, respectively, and modulation of the downstream molecular targets in human CWR22Rv1 prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CWR22Rv1 prostate cancer cells
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Concentration:5, 10, and 20 μM
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Incubation Time:24 h
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Result:Significantly and dose-dependently reduced the expressions of Mnk1, and peIF4E.
Caused significant depletion of the downstream target, cyclin D1, and induction of apoptosis via significant downregulation of antiapoptotic Bcl-2 and upregulation of proapoptotic Bax.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NRG mice (5-6 weeks) bearing CWR22Rv1 tumors[1]
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Dosage:24; 48; and 96 mg/kg
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Administration:p.o.; 5 days per/week; for 16 days
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Result:Caused a dose-dependent inhibition of tumor growth, with the two larger doses causing tumor regressions.
Inhibited tumor growth with TGIs of 147.5%, 136.8%, and 80.3%, at the dosage of 96, 48, and 24 mg/kg, respectively.
Chemical Information
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CAS No. 1239339-17-3
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Masse moléculaire 425.01
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Formule C26H33ClN2O
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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].Cl
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Synonyms
TOK-001 hydrochloride; VN-124-1 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Nature
2012 Jan 22;482(7383):116-9. PMID: 22266943 -
Drug Metab Dispos
Structural and Functional Evaluation of Clinically Relevant Inhibitors of Steroidogenic Cytochrome P450 17A1. [Abstract]2017 Jun;45(6):635-645. PMID: 28373265 -
Pureté et documentation
Références
[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. [Content Brief]
[2]. 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. Steroids. 2011 Nov;76(12):1268-79. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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