VNPP433-3β
Based on 1 Customer Validation
VNPP433-3β (Galeterone 3β-imidazole) 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 induces cell apoptosis. VNPP433-3β inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 1630820-51-7
- Formula: C29H34N4
- Molecular Weight:438.61
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
2.54 μM
Compound: 17
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Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay
Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay
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[PMID: 27437082] |
| LNCaP | EC50 |
190 nM
Compound: 17
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Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to control
Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to control
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[PMID: 27437082] |
| LNCaP | IC50 |
1.64 μM
Compound: 17
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Antiproliferative activity against human LNCAP cells after 7 days by MTT assay
Antiproliferative activity against human LNCAP cells after 7 days by MTT assay
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[PMID: 27437082] |
VNPP433-3β (compound 2) possess potent antiproliferative activities with GI50 of 0.2 μM, 0.3 μM, 0.31 μM against LNCaP (androgen-sensitive), C42B (androgen-insensitive) and CWR22Rv1 (castration-resistant), respectively[1].
VNPP433-3β (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: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 a TGI of 83.8%.
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. 1630820-51-7
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Appearance Solid
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Molecular Weight 438.61
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Formula C29H34N4
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Color Light yellow to yellow
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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
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Synonyms
Galeterone 3β-imidazole
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 10 mg/mL (22.80 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2799 mL | 11.3996 mL | 22.7993 mL | 56.9982 mL |
| 5 mM | 0.4560 mL | 2.2799 mL | 4.5599 mL | 11.3996 mL | |
| 10 mM | 0.2280 mL | 1.1400 mL | 2.2799 mL | 5.6998 mL | |
| 15 mM | 0.1520 mL | 0.7600 mL | 1.5200 mL | 3.7999 mL | |
| 20 mM | 0.1140 mL | 0.5700 mL | 1.1400 mL | 2.8499 mL |
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