2. PROTAC Vitamin D Related/Nuclear Receptor MAPK/ERK Pathway Apoptosis
  3. Molecular Glues Androgen Receptor MNK Apoptosis
  4. VNPP433-3β

VNPP433-3β  (Synonyms: Galeterone 3β-imidazole)

Cat. No.: HY-160777 Purity: 98.01%
COA
SDS
Handling Instructions Technical Support

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 proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and 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.

VNPP433-3β Chemical Structure

VNPP433-3β Chemical Structure

CAS No. : 1630820-51-7

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

VNPP433-3β Related Antibodies

Top Publications Citing Use of Products

View All MNK Isoform Specific Products:

View All Isoforms
MNK1 MNK2 MNK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and 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)[1].

In Vitro

VNPP433-3β 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[1].

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

VNPP433-3β 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

VNPP433-3β (20 mg/kg; p.o.; 5 days per/week; for 16 days) shows 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: 20 mg/kg
Administration: p.o.; 5 days per/week; for 16 days
Result: Caused a potent inhibition/regression of aggressive and difficult-to-treat CWR22Rv1 tumor xenografts growth, with no apparent host toxicities.
Molecular Weight

438.61

Formula

C29H34N4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2799 mL 11.3996 mL 22.7993 mL
5 mM 0.4560 mL 2.2799 mL 4.5599 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

VNPP433-3β Related Classifications

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:

VNPP433-3β1630820-51-7Galeterone 3β-imidazoleMolecular GluesAndrogen ReceptorMNKApoptosisMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseprostate cancerCRPCNRG mouseCD-1 mouseLNCaPC4-2BCWR22Rv1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
VNPP433-3β
Cat. No.:
HY-160777
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.