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Art. -Nr.: HY-70006A

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Galeterone hydrochloride

(Synonyms: TOK-001 hydrochloride; VN-124-1 hydrochloride)

3 Cited Publications

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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. Nr.: 1239339-17-3
Formel: C₂₆H₃₃ClN₂O
Molecular Weight:425.01

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (278 KB)

Galeterone hydrochloride Chemical Structure

CAS. Nr.: 1239339-17-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (3)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CYP17

47 nM (IC₅₀)

MNK1

MNK2

Alle MNK Isoform-spezifische Produkte anzeigen :

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

CWR22Rv1 prostate cancer cells
Concentration:

5, 10, and 20 μM
Incubation Time:

24 h
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.

Parmacokinetics

Species	Dose	Route	Note	C₀	T_1/2	AUC_0-last	C_max
Mice^[1]	1 mg/kg	i.v.	CD-1 male mice	98.34 ng/mL	1.02 h	44.34 ng·h/mL	/
Mice^[1]	10 mg/kg	p.o.	CD-1 male mice	/	5.16 h	26.06 ng·h/mL	10.49 ng/mL

In Vivo

Galeterone hydrochloride (24, 48, and 96 mg/kg; p.o.; 5 days per/week; for 16 days) shows dose-dependent antitumor activity in CWR22Rv1 tumor xenograft^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male NRG mice (5-6 weeks) bearing CWR22Rv1 tumors^[1]
Dosage:

24; 48; and 96 mg/kg
Administration:

p.o.; 5 days per/week; for 16 days
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

CAS. Nr. 1239339-17-3
Molecular Weight 425.01
Formel C₂₆H₃₃ClN₂O
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
Synonyms

TOK-001 hydrochloride; VN-124-1 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (3)

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Journal Impact Factor

Nature

Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001. [Abstract]

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
Patent

US20240400606A1.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Galeterone hydrochloride

3 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Reinheit & Dokumentation
Verweise

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Galeterone hydrochloride

Publications Citing Use of MedChemExpress (MCE) Galeterone hydrochloride

Alle MNK Isoform-spezifische Produkte anzeigen

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Galeterone hydrochloride Related Classifications

HY-70006A Related Classifications