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

目錄號(hào): HY-70006 純度: 99.87%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Galeterone (TOK-001) 是一種多功能的抗雄激素，是 CYP17 抑制劑，在去勢(shì)抵抗性前列腺癌中，IC₅₀ 為 47 nM。

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Galeterone Chemical Structure

CAS No. : 851983-85-2

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規(guī)格	價(jià)格	是否有貨
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	現(xiàn)貨	詢(xún)價(jià)
500 mg		詢(xún)價(jià)
1 g		詢(xún)價(jià)

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MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

•Nature. 2012 Jan 22;482(7383):116-9. [Abstract]
•Drug Metab Dispos. 2017 Jun;45(6):635-645. [Abstract]

Galeterone 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Cytochrome P450 亞型特異性產(chǎn)品:

查看所有亞型

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

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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

CYP17

細(xì)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]

體外研究
(In Vitro)

Galeterone (TOK-001) 提供強(qiáng) CYP17 裂解酶抑制作用，IC₅₀ 為 47 nM^[1]。Galeterone (TOK-001) 既是 CYP17A1 抑制劑又是雄激素受體拮抗劑，這些結(jié)合模式的相似性可能是這種雙重作用機(jī)制的原因。這種 CYP17A1 結(jié)合阿比特龍和 Galeterone (TOK-001)，吸光度在 402 nm 處降低并在 424 nm 處增加，這與氮與血紅素鐵的結(jié)合 (II 型相互作用) 一致，K_d 為 <100 nM^[2]。當(dāng) LNCaP 細(xì)胞在補(bǔ)充有活性炭剝離血清 (CSS，T<1 nM) 的培養(yǎng)基中培養(yǎng)，然后用增加濃度的 Galeterone (TOK-001) 處理時(shí)，AR 蛋白的穩(wěn)態(tài)水平顯著降低 (高達(dá) 84 %，15 μM Galeterone (TOK-001) )。在 LAPC-4 細(xì)胞中，阿比特龍醇在大于或等于 1 μM 的濃度下比 Galeterone (TOK-001) 更能降低 AR 表達(dá)。當(dāng) LNCaP 細(xì)胞用 20 μM TOK-001 處理 24 小時(shí)時(shí)，AR mRNA 水平降低了 38%^[3]。

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

體內(nèi)研究
(In Vivo)

接種 LAPC-4 腫瘤的小鼠每天兩次用 0.15 mmol/kg 的 Galeterone (TOK-001) 進(jìn)行皮下處理。與對(duì)照組相比，用 TOK-001 處理的小鼠在第 31 天的平均腫瘤體積更小 (p= 0.0001)。與對(duì)照相比，Galeterone (TOK-001) 處理還顯著降低了腫瘤生長(zhǎng)的增長(zhǎng)率 (p<0.0001)。切除后，與接受對(duì)照和閹割處理的動(dòng)物相比，接受 Galeterone (TOK-001) 處理的動(dòng)物的最終腫瘤重量也顯著降低 (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 號(hào)

851983-85-2

性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

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

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 25 mg/mL (64.34 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.43 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.43 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.43 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.87%

選擇批次：

Data Sheet (652 KB) SDS (419 KB)

COA (289 KB) LCMS (93 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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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滬ICP備15051369號(hào)-4

上海工商

滬公網(wǎng)安備31011502019417

滬(浦)應(yīng)急管危經(jīng)許[2021]201709(QFYS)

營(yíng)業(yè)執(zhí)照（三證合一）

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

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)