VNPP433-3β hydrochloride
VNPP433-3β (Galeterone 3β-imidazole) hydrochloride is an 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. VNPP433-3β hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
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- CAS No.: 3026905-91-6
- Formule: C29H35ClN4
- Masse moléculaire:475.07
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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
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
MNK1 |
MNK2 |
In Vitro
VNPP433-3β (compound 4) hydrochloride possess potent antiproliferative activities with GI50 of 0.28 μM, 0.33 μM, 0.26 μM against LNCaP (androgen-sensitive), C42B (androgen-insensitive) and CWR22Rv1 (castration-resistant), respectively[1].
VNPP433-3β (5-20 μM; 24 h) hydrochloride 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.
Parmacokinetics
In Vivo
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:5 and 20 mg/kg
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Administration:p.o.; 5 days per/week; for 16 days
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Result:Inhibited tumor growth with TGIs of 139.6 % at 20mg/kg, and 74.2% at 5 mg/kg.
Caused a potent inhibition/regression of aggressive and difficult-to-treat CWR22Rv1 tumor xenografts growth, with no apparent host toxicities.
Chemical Information
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CAS No. 3026905-91-6
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Masse moléculaire 475.07
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Formule C29H35ClN4
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SMILES
C[C@@]12[C@](CC=C2N3C4=CC=CC=C4N=C3)([H])[C@@]5([H])[C@]([C@@]6(C(C[C@@H](N7C=CN=C7)CC6)=CC5)C)([H])CC1.Cl
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Synonyms
Galeterone 3β-imidazole 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.
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VNPP433-3β hydrochloride Related Classifications
HY-160777B Related Classifications
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