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

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

Cat. No.: HY-160777A
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VNPP433-3β (Galeterone 3β-imidazole) dihydrochloride 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 dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).

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VNPP433-3β dihydrochloride

VNPP433-3β dihydrochloride Chemical Structure

CAS No. : 3026905-92-7

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VNPP433-3β dihydrochloride Related Antibodies

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Description

VNPP433-3β (Galeterone 3β-imidazole) dihydrochloride 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 dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC)[1].

In Vitro

VNPP433-3β (compound 5) dihydrochloride possess potent antiproliferative activities with GI50 of 0.23 μM, 0.21 μM, 0.28 μM against LNCaP (androgen-sensitive), C42B (androgen-insensitive) and CWR22Rv1 (castration-resistant), respectively[1].
VNPP433-3β dihydrochloride 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.

VNPP433-3β dihydrochloride Related Antibodies
In Vivo

VNPP433-3β (5 and 20 mg/kg; p.o.; 5 days per/week; for 16 days) dihydrochloride 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: 5 and 20 mg/kg
Administration: p.o.; 5 days per/week; for 16 days
Result: Inhibited tumor growth with TGIs of 152.9% at 20 mg/kg, and 79.2% at 5 mg/kg.
Caused a potent inhibition/regression of aggressive and difficult-to-treat CWR22Rv1 tumor xenografts growth, with no apparent host toxicities.
Molecular Weight

511.53

Formula

C29H36Cl2N4
CAS No.
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.Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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VNPP433-3β dihydrochloride 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:

VNPP433-3β3026905-92-7Galeterone 3β-imidazoleMolecular GluesAndrogen ReceptorMNKApoptosisMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseprostate cancerCRPCNRG mouseCD-1 mouseLNCaPC4-2BCWR22Rv1Inhibitorinhibitorinhibit

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