2. PROTAC Vitamin D Related/Nuclear Receptor MAPK/ERK Pathway Metabolic Enzyme/Protease Apoptosis
  3. Molecular Glues Androgen Receptor MNK Cytochrome P450 Apoptosis
  4. Galeterone hydrochloride

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

Cat. No.: HY-70006A
Handling Instructions Technical Support

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].

For research use only. We do not sell to patients.

Galeterone hydrochloride

Galeterone hydrochloride Chemical Structure

CAS No. : 1239339-17-3

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Galeterone hydrochloride Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

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].

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.

Galeterone hydrochloride Related Antibodies

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.
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.
Molecular Weight

425.01

Formula

C26H33ClN2O
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Galeterone hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Galeterone1239339-17-3TOK-001VN-124-1TOK001TOK 001Molecular GluesAndrogen ReceptorMNKCytochrome P450ApoptosisMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseCYPsmolecular glueARMAP kinaseMnk1/2CYP17prostate cancerxenograft mouse modelCRPCPDACInhibitorinhibitorinhibit

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