2. PROTAC Vitamin D Related/Nuclear Receptor MAPK/ERK Pathway Metabolic Enzyme/Protease Apoptosis
  3. Molecular Glues Androgen Receptor MNK Cytochrome P450 Apoptosis
  4. Galeterone hydrochloride

Galeterone hydrochloride  (Synonyms: TOK-001 hydrochloride; VN-124-1 hydrochloride)

目录号: HY-70006A
产品使用指南 技术支持

Galeterone (TOK-001) hydrochloride 是一种强效的口服活性分子胶 (molecular glue) 降解剂，可降解雄激素受体 (AR) 及其剪接变体 (AR-Vs) 以及 MAP 激酶相互作用的丝氨酸/苏氨酸蛋白激酶 Mnk1/2。Galeterone hydrochloride 具有 CYP17 抑制剂的作用 (IC50 = 47 nM)。Galeterone hydrochloride 诱导细胞凋亡 (apoptosis)。Galeterone hydrochloride 可抑制人前列腺癌异种移植小鼠模型中的肿瘤生长。Galeterone 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[1][2]。

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Galeterone hydrochloride

Galeterone hydrochloride Chemical Structure

CAS No. : 1239339-17-3

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Galeterone hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of Galeterone hydrochloride:

Galeterone hydrochloride 相关抗体

Top Publications Citing Use of Products

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Galeterone (TOK-001) hydrochloride is a potent, 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. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].

体外研究
(In Vitro)

Galeterone hydrochloride (compound 3) 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 0.36 μM、0.21 μM 和 0.56 μM[1]。
Galeterone hydrochloride (5-20 μM；24 小时) 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.

Galeterone 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)

Galeterone hydrochloride (24、48 和 96 mg/kg；口服；每周 5 天；共 16 天) 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: 24; 48; and 96 mg/kg
Administration: p.o.; 5 days per/week; for 16 days
Result: Caused a dose-dependent inhibition of tumor growth, with the two larger doses causing tumor regressions.
Inhibited tumor growth with TGIs of 147.5%, 136.8%, and 80.3%, at the dosage of 96, 48, and 24 mg/kg, respectively.
分子量

425.01

Formula

C26H33ClN2O
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

Galeterone hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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:

Galeterone1239339-17-3TOK-001VN-124-1TOK001TOK 001Molecular GluesAndrogen ReceptorMNKCytochrome P450ApoptosisMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseCYPsmolecular glueARMAP kinaseMnk1/2CYP17prostate cancerxenograft mouse modelCRPCPDACInhibitorinhibitorinhibit

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