化合物 Galeterone|T6509

Galeterone
851983-85-2

￥289 1mg 起订

￥678 5mg 起订

￥1080 10mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Galeterone

英文名称：: Galeterone

CAS号：: 851983-85-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.773%

产品类别：: 抑制剂

货号：: T6509

Product Introduction

Bioactivity

Name	Galeterone
Description	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.
Cell Research	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)
Kinase Assay	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.
In vitro	Galeterone在阻止[3H]-R1881与突变LNCaP AR (T877A)的结合方面有效，IC50为845 nM。Galeterone以剂量依赖性方式抑制DHT诱导的LNCaP和LAPC4细胞增殖，其IC50分别为6μM和3.2μM。[1] Galeterone还能抑制[3H]-R1881与PC3细胞中T575A突变AR的结合，IC50为454 nM。Galeterone在没有DHT刺激的情况下强效抑制LNCaP和LAPC4细胞增殖，其IC50分别为2.6μM和4μM。此外，Galeterone治疗以剂量依赖性方式增加AR降解率。[2] Galeterone强效抑制雄激素独立细胞系PC-3和DU-145的增长，以剂量依赖性方式，其GI50分别为7.82μM和7.55μM。Galeterone诱导内质网应激反应，导致cyclin D1蛋白表达下调和cyclin E2 mRNA下调。[3] Galeterone有效抑制HP-LNCaP和C4-2B细胞系的增殖，IC50分别为2.9μM和9.7μM。1μM的Galeterone治疗有效抑制LNCaP细胞（50%）和HP-LNCaP细胞（70%）的雄激素受体激活。Galeterone 1μM和411 nM的IC50分别降低LNCaP细胞和HP-LNCaP细胞的雄激素受体激活，并在24小时治疗后通过50%下调雄激素受体蛋白表达。[4] Galeterone降低AR蛋白和mRNA表达，对抗由雄激素诱导的AR依赖性启动子激活，并显著降低phospho-4EBP1水平。[6]
In vivo	给予Galeterone（50 mg/kg，每日两次）极其有效地抑制了依赖雄激素的LAPC4人类前列腺肿瘤异种移植物的生长，与对照组相比，最终平均肿瘤体积减少了93.8%，其效果也明显优于去势手术。[1] 通过每日两次给予Galeterone（0.13 mM/kg）或Galeterone（0.13 mmol/kg）加上去势手术，可以使SCID小鼠体内的LAPC4肿瘤异种移植物分别退缩26.55%和60.67%。Galeterone单独使用或结合去势治疗，分别可使AR蛋白的表达量显著降低10倍和5倍。[2]
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 19.4 mg/mL (50 mM) DMSO : 19.4 mg/mL (50 mM)
Keywords	CYPs \| Cytochrome P450 \| inhibit \| Galeterone \| Inhibitor \| TOK001 \| VN124 \| TOK 001 \| VN-124
Inhibitors Related	Naringin \| 1-Aminobenzotriazole \| Fenofibrate \| Tauroursodeoxycholate \| Flutamide \| Methoxsalen \| Naringenin \| Apigenin \| 1-Ethynylnaphthalene \| Dehydroisoandrosterone 3-acetate \| Tebuconazole \| Diflubenzuron
Related Compound Libraries	Inhibitor Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Anti-Aging Compound Library \| Nuclear Receptor Compound Library \| Drug Repurposing Compound Library \| Anti-Metabolism Disease Compound Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

VN-124-1|||VN/124-1|||VN 124|||TOK-001|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子