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

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

目录号: HY-160777B
产品使用指南 技术支持

VNPP433-3β (Galeterone 3β-imidazole) hydrochloride 是一种口服有效的分子胶 (molecular glue) 降解剂，可靶向降解雄激素受体 (AR) 及其剪接变体 (AR-Vs) 和与 MAP 激酶相互作用的丝氨酸/苏氨酸蛋白激酶 Mnk1/2。VNPP433-3β hydrochloride 诱导细胞凋亡 (apoptosis)。VNPP433-3β hydrochloride 抑制异种移植小鼠模型中 CWR22Rv1 肿瘤生长。VNPP433-3β hydrochloride 可用于去势抵抗性前列腺癌 (CRPC) 和胰腺导管腺癌 (PDAC) 的研究。

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VNPP433-3β hydrochloride

VNPP433-3β hydrochloride Chemical Structure

CAS No. : 3026905-91-6

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VNPP433-3β hydrochloride 的其他形式现货产品:

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VNPP433-3β hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)[1].

体外研究
(In Vitro)

VNPP433-3β (compound 4) hydrochloride 具有强大的抗增殖活性，对 LNCaP (雄激素敏感)、C42B (雄激素不敏感) 和 CWR22Rv1 (去势抵抗) 的 GI50 分别为 0.28 μM、0.33 μM 和 0.26 μM[1]。
VNPP433-3β (5-20 μM；24 小时) hydrochloride 在人类 CWR22Rv1 前列腺癌细胞中可降解 AR/AR-V7 和 Mnk1/2，从而分别抑制 AR 信号传导和消耗 peIF4E，并调节下游分子靶点[1]。

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

VNPP433-3β hydrochloride 相关抗体:

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.
体内研究
(In Vivo)

VNPP433-3β (5 和 20 mg/kg；口服；每周 5 天；共 16 天) hydrochloride 在 CWR22Rv1 肿瘤异种移植瘤中显示出抗肿瘤活性[1]。

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 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.
分子量

475.07

Formula

C29H35ClN4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

VNPP433-3β hydrochloride 相关分类

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  • 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:

VNPP433-3β3026905-91-6Galeterone 3β-imidazoleMolecular GluesAndrogen ReceptorMNKApoptosisMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseprostate cancerCRPCNRG mouseCD-1 mouseLNCaPC4-2BCWR22Rv1Inhibitorinhibitorinhibit

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