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Abiraterone/阿比特龙 {[allProObj[0].p_purity_real_show]}

货号:A515845 同义名: CB-7598

Abiraterone是一种强效的CYP17A1抑制剂,IC50为4 nM。

Abiraterone/阿比特龙 化学结构 CAS号:154229-19-3
Abiraterone/阿比特龙 化学结构
CAS号:154229-19-3
Abiraterone/阿比特龙 3D分子结构
CAS号:154229-19-3
Abiraterone/阿比特龙 化学结构 CAS号:154229-19-3
Abiraterone/阿比特龙 3D分子结构 CAS号:154229-19-3
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Abiraterone/阿比特龙 纯度/质量文件 产品仅供科研

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Abiraterone/阿比特龙 生物活性

描述 The 17α-hydroxylase/C17-20 lyase (as known as CYP17A1) is a key enzyme in the androgen biosynthetic pathway. Abiraterone is a potent inhibitor of both 17α-hydroxylase and C17-20 lyase with IC50 values of 18 and 17 nM, respectively[4]. In guinea pig adrenal cells, abiraterone at the dose of 10-5 M almost completely inhibited ACTH-stimulated production of androstenedione and cortisol[5]. Moreover, abiraterone is also an inhibitor of androgen receptor (AR). It displaced ligand from wild-type AR with an EC50 value of 13.4 μM. Abiraterone (0.1 - 25 μM) also showed dose-proportional inhibitory effect on T877A-AR, G142VAR, P533S-AR, T575A-AR and H874Y-AR. In LNCaP and VCaP prostate cancer cells. Abiraterone at the concentrations of 0.1 - 5 μM decreased cell viability in a dose-dependent manner when compared to DMSO control[6]. After the treatment of LuCaP23CR and LuCaP35CR prostate cancer xenografts with abiraterone for 21 days, the serum PSA level was rapidly declined and the tumor growth was significantly inhibited as compared to vehicle-treated group. Abiraterone administration also resulted in statistically significant improvement in the progression-free survival[7].

Abiraterone/阿比特龙 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
hamster V79MZh11B1 cells Function assay Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=1.608 μM 18672868
PC3 cells Cytotoxic assay 48 h Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=9.32 μM 24148837

Abiraterone/阿比特龙 动物研究

Dose Mice: 200 mg/kg[3]
Administration p.o.

Abiraterone/阿比特龙 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01017939 Prostate Neoplasms Phase 1 Completed - United States, California ... 展开 >> Tower Cancer Research Foundation Beverly Hills, California, United States, 90211 Beverly Hills, California, United States United States, Texas START - South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 San Antonio, Texas, United States Canada, British Columbia BC Cancer Agency Vancouver, British Columbia, Canada, V5Z 4E6 Vancouver, British Columbia, Canada 收起 <<
NCT03748641 Metastatic Prostate Cancer Phase 3 Not yet recruiting February 25, 2025 -
NCT02090114 Prostate Cancer Phase 2 Recruiting April 2019 United States, Maryland ... 展开 >> The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Recruiting Baltimore, Maryland, United States, 21231 Contact: Irina Rifkind, RN, MSN    410-502-2043    irifkin1@jhmi.edu    Contact: Rana Sullivan, RN, BSN    410-614-6337    tomalra@jhmi.edu    Principal Investigator: Samuel Denmeade, MD 收起 <<

Abiraterone/阿比特龙 参考文献

[1]Richards J, Lim AC, et al. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82.

[2]Attard G, Reid AH, et al. Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that castration-resistant prostate cancer commonly remains hormone driven. J Clin Oncol. 2008 Oct 1;26(28):4563-71.

[3]Liu C, Armstrong C, et al. Niclosamide enhances abiraterone treatment via inhibition of androgen receptor variants in castration resistant prostate cancer. Oncotarget. 2016;7(22):32210-20.

[4]Potter GA, Barrie SE, Jarman M, Rowlands MG. Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer. J Med Chem. 1995 Jun 23;38(13):2463-71. doi: 10.1021/jm00013a022. PMID: 7608911.

[5]Barrie SE, Potter GA, Goddard PM, Haynes BP, Dowsett M, Jarman M. Pharmacology of novel steroidal inhibitors of cytochrome P450(17) alpha (17 alpha-hydroxylase/C17-20 lyase). J Steroid Biochem Mol Biol. 1994 Sep;50(5-6):267-73. doi: 10.1016/0960-0760(94)90131-7. PMID: 7918112.

[6]Richards J, Lim AC, Hay CW, Taylor AE, Wingate A, Nowakowska K, Pezaro C, Carreira S, Goodall J, Arlt W, McEwan IJ, de Bono JS, Attard G. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82. doi: 10.1158/0008-5472.CAN-11-3980. Epub 2012 Mar 12. PMID: 22411952; PMCID: PMC4281708.

[7]Mostaghel EA, Marck BT, Plymate SR, Vessella RL, Balk S, Matsumoto AM, Nelson PS, Montgomery RB. Resistance to CYP17A1 inhibition with abiraterone in castration-resistant prostate cancer: induction of steroidogenesis and androgen receptor splice variants. Clin Cancer Res. 2011 Sep 15;17(18):5913-25. doi: 10.1158/1078-0432.CCR-11-0728. Epub 2011 Aug 1. PMID: 21807635; PMCID: PMC3184252.

Abiraterone/阿比特龙 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.61mL

5.72mL

2.86mL

Abiraterone/阿比特龙 技术信息

CAS号154229-19-3
分子式C24H31NO
分子量 349.51
SMILES Code [H][C@@]12CC=C(C3=CC=CN=C3)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC=C2C[C@@H](O)CC[C@]12C
MDL No. MFCD00924100
别名 CB-7598
运输蓝冰
InChI Key GZOSMCIZMLWJML-VJLLXTKPSA-N
Pubchem ID 132971
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 2 mg/mL(5.72 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 5 mg/mL(14.31 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

DMF: 8 mg/mL(22.89 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 60 mg/mL suspension

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