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)

製品番号: HY-160777 純度: 98.01%
COA 取扱説明書 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 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).

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VNPP433-3β

VNPP433-3β 構造式

CAS 番号 : 1630820-51-7

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1320 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1320 在庫あり
Solid
1 mg $540 在庫あり
5 mg $1200 在庫あり
10 mg $2000 在庫あり
25 mg $4000 在庫あり
50 mg $6400 在庫あり
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VNPP433-3β 関連抗体

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製品説明

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)[1].

Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
2.54 3
Compound: 17
Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay
Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay
[PMID: 27437082]
CWR22R IC50
2.54 3
Compound: 17
Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay
Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay
[PMID: 27437082]
LNCaP EC50
190 1
Compound: 17
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
[PMID: 27437082]
LNCaP IC50
1.64 3
Compound: 17
Antiproliferative activity against human LNCAP cells after 7 days by MTT assay
Antiproliferative activity against human LNCAP cells after 7 days by MTT assay
[PMID: 27437082]
LNCaP IC50
1.64 3
Compound: 17
Antiproliferative activity against human LNCAP cells after 7 days by MTT assay
Antiproliferative activity against human LNCAP cells after 7 days by MTT assay
[PMID: 27437082]
LNCaP EC50
190 1
Compound: 17
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
[PMID: 27437082]
体外実験

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.

VNPP433-3β 関連抗体

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.
体内実験

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: 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.
分子量

438.61

分子式

C29H34N4
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外: 

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
10 mM 0.2280 mL 1.1400 mL 2.2799 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.

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一般には略語で表示されます：C1V1 = C2V2

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純度とドキュメンテーション
参考文献

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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VNPP433-3β Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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

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