Abiraterone

別名：CB-7598

製品コード：S1123 純度：99.98%

Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.

CAS No. 154229-19-3

サイズ	価格(税別)	在庫状況
5mg	JPY 25500	国内在庫あり
25mg	JPY 55500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（32）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Abiraterone関連製品

関連ターゲット	P450 CYP2 CYP51 CYP3 CYP735 CYP11 CYP26 CYP2C9 CYP1 CYP17	もっと見る
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シグナル伝達経路

P450 (e.g. CYP17)シグナル伝達経路

P450 (e.g. CYP17)阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
LNCAP	Antiproliferative assay	72 hrs	Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay, IC50=3.29μM.	29310026
hTERT-BJ	Cytotoxicity assay	48 hrs	Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay, GI50=4.5μM.	29172080
PC3	Antiproliferative assay	72 hrs	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50=5.94μM.	29310026
MGC803	Antiproliferative assay	72 hrs	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay, IC50=7.72μM.	29310026
HeLa	Antiproliferative assay	48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50=7.9μM.	29172080
PC3	Cytotoxicity assay	48 hrs	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=9.32μM.	24148837
GES-1	Antiproliferative assay	72 hrs	Antiproliferative activity against human GES-1 cells after 72 hrs by MTT assay, IC50=13.12μM.	29310026
T47D	Growth inhibition assay	72 hrs	Growth inhibition of human T47D cells after 72 hrs by MTT assay, IC50=16.9μM.	27209562
MDA-MB-231	Growth inhibition assay	72 hrs	Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=19.2μM.	27209562
MCF7	Growth inhibition assay	72 hrs	Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50=19.3μM.	27209562
MDA-MB-361	Growth inhibition assay	72 hrs	Growth inhibition of human MDA-MB-361 cells after 72 hrs by MTT assay, IC50=20.4μM.	27209562
T47D	Antiproliferative assay	48 hrs	Antiproliferative activity against human T47D cells after 48 hrs by SRB assay, GI50=24μM.	29172080
WiDr	Antiproliferative assay	48 hrs	Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay, GI50=42μM.	29172080
JM109	Growth inhibition assay		Inhibition of C-terminal His-tagged recombinant human CYP17A1delta19H mutant expressed in Escherichia coli JM109 cells assessed as decrease in progesterone hydroxylation in presence of cytochrome P450 reductase by HPLC-UV method, IC50=0.0094μM.	29792703
P450c17-LNCaP	Growth inhibition assay		In vitro cytochrome P450 17A1 inhibition was assayed using the rapid acetic acid releasing assay (AARA), utilizing intact P450c17-expressing Escherichia coli or P450c17-LNCaP cells as the enzyme source, IC50=0.8μM.	12773039
V79MZh11B1	Growth inhibition assay		Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=1.608μM.	18672868
V79MZh11B1	Growth inhibition assay		Inhibition of recombinant CYP11B1 expressed in expressed in V79MZh11B1 cells, IC50=1.608μM.	19211174
V79MZh	Growth inhibition assay		Inhibition of human CYP11B1 expressed in hamster V79MZh cells, IC50=1.61μM.	20550118
V79MZh	Growth inhibition assay		Inhibition of human CYP11B1 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate, IC50=1.61μM.	23859149
V79MZh	Growth inhibition assay		Inhibition of human CYP11B2 expressed in hamster V79MZh cells, IC50=1.75μM.	20550118
V79MZh	Growth inhibition assay		Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate, IC50=1.75μM.	23859149
V79MZh11B2	Growth inhibition assay		Inhibition of human CYP11B2 expressed in hamster V79MZh11B2 cells, IC50=1.751μM.	18672868
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生物活性

製品説明

Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.

特性

Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.

Targets

CYP17 ^[1]
(Cell-free assay)

2 nM

In Vitro
In vitro	Abiraterone binds and inhibits wild-type and mutant androgen receptor (AR). Abiraterone inhibits in vitro proliferation and androgen receptor-regulated gene expression of androgen receptor-positive prostate cancer cells, which could be explained by androgen receptor antagonism in addition to inhibition of steroidogenesis. In fact, activation of mutant androgen receptor by eplerenone is inhibited by greater concentrations of Abiraterone. Abiraterone displaces ligand from both WT-AR and T877A with EC50 of 13.4 μM and 7.9 μM, respectively. ^[2]Abiraterone inhibits lyase activity with an IC50 of 5.8 nM in rat testis microsomes. Abiraterone acetate significantly inhibits T secretion (−48%) and in turn increased LH concentration (192%).^[3]
Kinase Assay	C_17,20-lyase activity assay
Kinase Assay	Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contained 0.25 M sucrose, 20 mM Tris–HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, Abiraterone is evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at −20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format using a specific antibody against Δ4A. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a 1450 MicrobetaPlus liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration.
細胞実験	細胞株	LNCaP and VCaP cells
	濃度	0.1-5 μM
	反応時間	24 hours or 96 hours
	実験の流れ	LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	eIF4E / eIF4G / eIF4E / eIF4G / AR p-4EBP1 / 4EBP1		22174412

In Vivo
In Vivo	Abiraterone inhibits CYP17 with an IC50 of 72 nM, in human testicular microsomes. ^[4] Abiraterone fails to significantly reduce the size of any of the organs. ^[5] Abiraterone reduces the testosterone levels strongly, almost reaching the level of the orchiectomy control. The testosterone levels are reduced by Abiraterone for more than 95% compared to the control group. ^[6]
動物実験	動物モデル	LAPC-4 xenograft mice
	投与量	0.15 mmol/kg
	投与経路	Administered via s.c.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06014853	Completed	Prostate Cancer	Bukwang Pharmaceutical\|Dyna Therapeutics	August 10 2023	Phase 1
NCT03348670	Active not recruiting	Prostate Cancer	Han Xu M.D. Ph.D. FAPCR Sponsor-Investigator IRB Chair\|Medicine Invention Design Inc	August 18 2023	Phase 2\|Phase 3
NCT05737082	Completed	Healthy	Hanmi Pharmaceutical Company Limited	March 30 2023	Phase 1

参考
[1] Attard G, et al. J Clin Oncol. 2008, 26(28), 4563-4571. [2] Richards J, et al. Cancer Res. 2012, 72(9), 2176-2182. [3] Duc I, et al. J Steroid Biochem Mol Biol. 2003, 84(5), 537-542. [4] Hu Q, et al. J Med Chem. 2010, 53(15), 5749-5758. [5] Bruno RD, et al. Steroids. 2011, 76(12), 1268-1279. [6] Haidar S, et al. J Steroid Biochem Mol Biol. 2003, 84(5),555-562. + 展開

参考

+ 展開

化学情報

分子量	349.51	化学式	C₂₄H₃₁NO
CAS No.	154229-19-3	SDF	Download Abiraterone SDFをダウンロードする
Smiles	CC12CCC(CC1=CCC3C2CCC4(C3CC=C4C5=CN=CC=C5)C)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

tert-Butanol : 6 mg/mL

DMSO : 0.33 mg/mL ( (0.94 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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