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Galeterone

Galeterone

产品编号 T6509   CAS 851983-85-2
别名: VN-124-1, TOK-001, VN/124-1, VN 124

Galeterone (VN 124) 是CYP17抑制剂,能够多功能的抗雄激素,在去势抵抗性前列腺癌中,其IC50值为 47 nM。

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Galeterone Chemical Structure
Galeterone, CAS 851983-85-2
规格 价格/CNY 货期 数量
1 mg ¥ 289 现货
5 mg ¥ 678 现货
10 mg ¥ 1,080 现货
25 mg ¥ 1,890 现货
50 mg ¥ 2,970 现货
100 mg ¥ 4,580 现货
200 mg ¥ 6,530 现货
1 mL * 10 mM (in DMSO) ¥ 747 现货
产品目录号及名称: Galeterone (T6509)
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纯度: 99.773%
纯度: 99.57%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.
靶点活性 Androgen Receptor:384 nM, CYP17:300 nM
体外活性 Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) with IC50 of 845 nM. Galeterone inhibits the DHT-induced proliferation of LNCaP and LAPC4 cells in a dose-dependent manner with IC50 of 6 μM and 3.2 μM, respectively. [1] Galeterone also inhibits the binding of [3H]-R1881 to the T575A mutant AR in PC3 cells with IC50 of 454 nM. Galeterone potently inhibits the proliferation of LNCaP and LAPC4 cells in the absence of DHT stimulation with IC50 of 2.6 μM and 4 μM, respectively. Furthermore, Galeterone treatment increases the degradation rate of the AR in a dose-dependent manner. [2] Galeterone potently inhibits the growth of the androgen-independent cell lines PC-3 and DU-145 in a dose-dependent manner with GI50 of 7.82 μM and 7.55 μM, respectively. Galeterone induces the endoplasmic reticulum stress response resulting in down-regulation of cyclin D1 protein expression and cyclin E2 mRNA. [3] Galeterone effectively inhibits proliferation of HP-LNCaP and C4-2B cell lines with IC50 of 2.9 μM and 9.7 μM, respectively. Galeterone treatment at 1 μM effectively inhibits androgen receptor activation in LNCaP cells (50%) and HP-LNCaP cells (70%). Galeterone decreases activation of the androgen receptor in both LNCaP cells and HP-LNCaP cells with IC50 of 1 μM and 411 nM, respectively, and down-regulates androgen receptor protein expression by 50% after 24 hour of treatment. [4] Galeterone reduces AR protein and mRNA expression, antagonizes AR-dependent promoter activation induced by androgen, and significantly reduces the phospho-4EBP1 levels. [6]
体内活性 Administration of Galeterone at 50 mg/kg twice daily is very effective at inhibiting the growth of androgen-dependent LAPC4 human prostate tumor xenograft, with a 93.8% reduction in the mean final tumor volume compared with controls, and it is also significantly more effective than castration. [1] Treatment of Galeterone (0.13 mM/kg twice daily) or Galeterone (0.13 mmol/kg twice daily) plus castration induces regression of LAPC4 tumor xenografts in SCID mice by 26.55% and 60.67%, respectively. Treatments with Galeterone or Galeterone plus castration causes marked reduction in AR protein of 10- and 5-fold, respectively. [2]
激酶实验 In vitro assay of CYP17: The in vitro CYP17 inhibitory activity of Galeterone is evaluated using rapid acetic acid releasing assay (AARA), utilizing intact P450c17-expressing E. coli as the enzyme source. It involves the use of [21-3H]-17α-hydroxypregnenolone as the substrate, and CYP17 activity is measured by the amount of tritiated acetic acid formed during the cleavage of the C-21 side chain of the substrate. IC50 value is obtained directly from plots relating percentage inhibition versus inhibitor concentration over appropriate ranges.
细胞实验 Cells are seeded in 24 well multi-well plates. Cells are treated with the increasing concentration of Galeterone in steroid free medium with or without 1 nM DHT (LNCaP), or 10 nM DHT (LAPC4) and allowed to grow for 7 days. The number of viable cells is compared by MTT assay (LAPC4) or XTT assay (LNCaP) on the 7th day. (Only for Reference)
别名 VN-124-1, TOK-001, VN/124-1, VN 124
分子量 388.55
分子式 C26H32N2O
CAS No. 851983-85-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 19.4 mg/mL (50 mM)

DMSO: 19.4 mg/mL (50 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / 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
20 mM 0.1287 mL 0.6434 mL 1.2868 mL 3.2171 mL
50 mM 0.0515 mL 0.2574 mL 0.5147 mL 1.2868 mL

计算器

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稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Handratta VD, et al. J Med Chem, 2005, 48(8), 2972-2984. 2. Vasaitis T, et al. Mol Cancer Ther, 2008, 7(8), 2348-2357. 3. Bruno RD, et al. Mol Cancer Ther, 2008, 7(9), 2828-2836. 4. Schayowitz A, et al. Mol Cancer Ther, 2008, 7(1), 121-132. 5. Schayowitz A, et al. Br J Cancer, 2010, 103(7), 12001-12007.
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相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 抗癌临床化合物库 抗衰老化合物库 核受体化合物库 临床期小分子药物库 抗代谢疾病化合物库 内质网应激化合物库 抑制剂库 经典已知活性库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Galeterone 851983-85-2 Endocrinology/Hormones Metabolism P450 Androgen Receptor CYPs Cytochrome P450 VN-124-1 inhibit TOK-001 Inhibitor VN/124-1 TOK001 VN 124 VN124 TOK 001 VN-124 inhibitor

 

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