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

目录号: HY-70006 纯度: 99.87%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Galeterone (TOK-001) 是一种多功能的抗雄激素，是 CYP17 抑制剂，在去势抵抗性前列腺癌中，IC₅₀ 为 47 nM。

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Galeterone Chemical Structure

CAS No. : 851983-85-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥701	In-stock
1 mg	￥361	In-stock
5 mg	￥820	In-stock
10 mg	￥1300	In-stock
25 mg	￥2363	In-stock
50 mg	￥3700	In-stock
100 mg	￥5920	In-stock
200 mg	现货	询价
500 mg		询价
1 g		询价

or 大包装询价

* Please select Quantity before adding items.

MCE 顾客使用本产品发表的 2 篇科研文献

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查看所有亚型

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

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC₅₀=47 nM) in castration resistant prostate cancer (CRPC).

IC₅₀ & Target

IC50: 47 nM (CYP17)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	GI₅₀	3.9 μM Compound: Galeterone	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay Antiproliferative activity against human A549 cells after 48 hrs by SRB assay	[PMID: 29172080]
CWR22R	GI₅₀	37.8 μM Compound: Galeterone	Antiproliferative activity against AR-positive human 22Rv1 cells harboring ARE14 construct assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human 22Rv1 cells harboring ARE14 construct assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
CWR22R	IC₅₀	8.91 μM Compound: 5; Galeterone	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]
HBL-100	GI₅₀	10 μM Compound: Galeterone	Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay	[PMID: 29172080]
HeLa	GI₅₀	5.3 μM Compound: Galeterone	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay	[PMID: 29172080]
hTERT-BJ	GI₅₀	5 μM Compound: Galeterone	Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay	[PMID: 29172080]
LNCaP	GI₅₀	3.35 μM Compound: 5, TOK-001, Galeterone	Cytotoxicity against human LNCAP cells after 7 days by MTT assay Cytotoxicity against human LNCAP cells after 7 days by MTT assay	[PMID: 23713567]
LNCaP	IC₅₀	3.93 μM Compound: 5; Galeterone	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	3548 nM Compound: 6; TOK-001, VN/124-1	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay	[PMID: 36070471]
LNCaP	EC₅₀	670 nM Compound: 5, TOK-001, Galeterone	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis	[PMID: 23713567]
LNCaP C4-2	GI₅₀	> 40 μM Compound: Galeterone	Antiproliferative activity against AR-positive human C4-2 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human C4-2 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
PC-3	GI₅₀	37.7 μM Compound: Galeterone	Antiproliferative activity against AR-negative human PC3 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-negative human PC3 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
SW1573	GI₅₀	3.9 μM Compound: Galeterone	Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay	[PMID: 29172080]
T47D	GI₅₀	2.1 μM Compound: Galeterone	Antiproliferative activity against human T47D cells after 48 hrs by SRB assay Antiproliferative activity against human T47D cells after 48 hrs by SRB assay	[PMID: 29172080]
VCaP	GI₅₀	> 40 μM Compound: Galeterone	Antiproliferative activity against AR-positive human VCaP cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human VCaP cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
WiDr	GI₅₀	2.7 μM Compound: Galeterone	Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay	[PMID: 29172080]

体外研究
(In Vitro)

Galeterone (TOK-001) affords strong CYP17 lyase inhibition, with IC₅₀ of 47 nM^[1]. Galeterone (TOK-001) is both a CYP17A1 inhibitor and androgen receptor antagonist and the similarity of these binding modes is likely the reason for this dual mechanism of action.This CYP17A1 binds abiraterone and Galeterone (TOK-001) with absorbance decreases at 402 nm and increases at 424 nm, consistent with nitrogen binding to the heme iron (type II interaction) with K_d of <100 nM^[2]. When LNCaP cells are cultured in medium supplemented with charcoal-stripped serum (CSS, T<1 nM) followed by treatment with increasing concentrations of Galeterone (TOK-001), the steady-state levels of AR protein are markedly decreased (up to 84%, 15 μM Galeterone (TOK-001)). In LAPC-4 cells, abiraterone alcohol reduced AR expression to a greater extent than Galeterone (TOK-001) at concentrations greater than or equal to 1 μM. When LNCaP cells are treated with 20 μM TOK-001 for 24 h, AR mRNA levels are reduced by 38%^[3].

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

体内研究
(In Vivo)

Mice inoculated with LAPC-4 tumors are treated subcutaneously with 0.15 mmol/kg of Galeterone (TOK-001) twice daily. Mice treated with TOK-001 have smaller average tumor volume on day 31 when compared to control (p= 0.0001). Galeterone (TOK-001) treatment also significantly reduces the growth rate of tumor growth compared to control (p<0.0001). Upon excision, final tumor weights are also significantly reduced in animals treated with Galeterone (TOK-001) compared to animals treated with control, and castration (p<0.05)^[1].

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

Clinical Trial

分子量

388.55

Formula

C₂₆H₃₂N₂O

CAS 号

851983-85-2

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (64.34 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5737 mL	12.8684 mL	25.7367 mL
5 mM	0.5147 mL	2.5737 mL	5.1473 mL
10 mM	0.2574 mL	1.2868 mL	2.5737 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.87%

选择批次：

Data Sheet (630 KB) SDS (419 KB)

COA (289 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Bruno RD, et al. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.Steroid [Content Brief]

[2]. DeVore NM, et al. Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001.Nature. 2012 Jan 22;482(7383):116-9. [Content Brief]

[3]. Soifer HS, et al. Direct regulation of androgen receptor activity by potent CYP17 inhibitors in prostate cancer cells.J Biol Chem. 2012 Feb 3;287(6):3777-87. Epub 2011 Dec 15. [Content Brief]

Cell Assay ^[3]	LNCaP cells are seeded in 24-well plates at 70% confluence a day before transfections. Cells then are transfected with plasmid DNA (0.5 μg/well) carrying pIR-AR 5′UTR-Luc (5′UTR; test) or pIRES-Luc (IRES, control) for 6 h in serum-free and antibiotic-free conditions. Transcription of both luciferase reporter genes is under the control of the CMV promoter. Lipofectamine 2000 reagent is used in all transfections according to the manufacturer's instructions. Cells are then treated with doses of Galeterone (TOK-001) (0, 10, and 20 μM) in 5% FBS/T-Medium. Luciferase reporter gene activities are measured using Luciferase Assay System from Promega at 36 h post treatment using a BMG Labtech microplate reader. Relative luciferase units are normalized to total protein and then normalized to vector control (pIR-AR 5′UTR-Luc) and the result is presented as luciferase activity. For cell proliferation studies, LNCaP cells in 96-well plate are seeded 24 h prior to drug treatment and then treated with control (mock), Galeterone (TOK-001) (10 μM), or abiraterone alcohol (10 μM) in 5% FBS/T-medium for 72 h. Cell proliferation is determined using MTS^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Mice inoculated with LAPC-4 tumors are treated subcutaneously with 0.15 mmol/kg of Galeterone (TOK-001) twice daily. Mice treated with TOK-001 have smaller average tumor volume on day 31 when compared to control (p=0.0001). Galeterone (TOK-001) treatment also significantly reduced the growth rate of tumor growth compared to control (p<0.0001). Upon excision, final tumor weights are also significantly reduced in animals treated with Galeterone (TOK-001) compared to animals treated with control, and castration (p<0.05). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Bruno RD, et al. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.Steroid [Content Brief] [2]. DeVore NM, et al. Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001.Nature. 2012 Jan 22;482(7383):116-9. [Content Brief] [3]. Soifer HS, et al. Direct regulation of androgen receptor activity by potent CYP17 inhibitors in prostate cancer cells.J Biol Chem. 2012 Feb 3;287(6):3777-87. Epub 2011 Dec 15. [Content Brief]

Galeterone 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5737 mL	12.8684 mL	25.7367 mL	64.3418 mL
	5 mM	0.5147 mL	2.5737 mL	5.1473 mL	12.8684 mL
	10 mM	0.2574 mL	1.2868 mL	2.5737 mL	6.4342 mL
	15 mM	0.1716 mL	0.8579 mL	1.7158 mL	4.2895 mL
	20 mM	0.1287 mL	0.6434 mL	1.2868 mL	3.2171 mL
	25 mM	0.1029 mL	0.5147 mL	1.0295 mL	2.5737 mL
	30 mM	0.0858 mL	0.4289 mL	0.8579 mL	2.1447 mL
	40 mM	0.0643 mL	0.3217 mL	0.6434 mL	1.6085 mL
	50 mM	0.0515 mL	0.2574 mL	0.5147 mL	1.2868 mL
	60 mM	0.0429 mL	0.2145 mL	0.4289 mL	1.0724 mL

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:

Galeterone851983-85-2TOK-001 VN-124-1TOK001TOK 001Cytochrome P450CYPsInhibitorinhibitorinhibit

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

MCE 顾客使用本产品发表的 2 篇科研文献

Galeterone 相关产品

•相关化合物库:

•同靶点产品:

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查看 Cytochrome P450 亚型特异性产品:

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实验参考方法

纯度 & 产品资料

参考文献

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完整储备液配制表

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

Galeterone 相关抗体

MCE 顾客使用本产品发表的 2 篇科研文献

Galeterone 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Cytochrome P450 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Galeterone 相关抗体:

摩尔计算器

稀释计算器

Galeterone 相关分类

完整储备液配制表

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