Abiraterone

製品コードS1123 別名:CB-7598

Abiraterone化学構造

分子量(MW):349.51

Abirateroneは、2nMのIC50による強力なCYP17阻害剤です。

サイズ 価格(税別)  
JPY 28220.00
JPY 94620.00

カスタマーフィードバック(2)

  • A. ZR75-1 (AR+, ER+) and B. MDA MB 231 (AR-, TNBC) cells were treated with either abiraterone or vehicle, then used as targets in a CTL assay using CEA-specific CD8+ T cells as effector cells at an E:T ratio of 30:1. Error bars indicate mean ± S.E.M. for quadruplicate measurements. Statistical analyses were done by Student's t-test, * = P < 0.01 vs. vehicle control. Data are representative of 2 independent experiments.

    Oncotarget, 2016, 7(17):23498-511. Abiraterone purchased from Selleck.

    Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.

    Prostate 2013 74, 235-49. Abiraterone purchased from Selleck.

製品安全説明書

P450 (e.g. CYP17)阻害剤の選択性比較

生物活性

製品説明 Abirateroneは、2nMのIC50による強力なCYP17阻害剤です。
特性 Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.
ターゲット
CYP17 [1]
(Cell-free assay)
2 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
hamster V79MZh11B1 cells M3[1VGZ2dmO2aX;uJIF{e2G7 NUTxN2k6UW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcDFzQkGgZ4VtdHNuIFnDOVA:OS54MEig{txO MkLzNVg3PzJ6Nki=
PC3 cells MmnzR5l1d3SxeHnjxsBie3OjeR?= NHnDN4Q1QCCq M2nlb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvOzJizszN MorwNlQyPDh6M{e=

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[3]
+ 展開

C17,20-lyase activity 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.
細胞試験: [2]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[5]
+ 展開
  • 動物モデル: LAPC-4 xenograft mice
  • 製剤: 0.3% hydroxypropyl cellulose
  • 投薬量: 0.15 mmol/kg
  • 投与方法: Administered via s.c.
    (参考用のみ)

溶解度 (25°C)

体外 DMF 4 mg/mL (11.44 mM) warming
Ethanol 0.2 mg/mL (0.57 mM)
DMSO 0.1 mg/mL (0.28 mM)

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 349.51
化学式

C24H31NO

CAS No. 154229-19-3
保管
別名 CB-7598

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01553188 Active, not recruiting Prostatic Neoplams|Prostate Cancer|Neoplasm, Prostate|Neoplasm,Prostatic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 7, 2012 Phase 2
NCT02403505 Not yet recruiting Stage, Prostate Cancer|Surgery Dr. Han Xu, President/CEO / PD / PI / Monitor / IRB Chair|PPD|Medicine Invention Design, Inc August 2020 Phase 3
NCT02949284 Not yet recruiting Stage II Prostate Adenocarcinoma|Stage III Prostate Adenocarcinoma Rutgers, The State University of New Jersey|National Cancer Institute (NCI) June 2017 Phase 2
NCT02987543 Recruiting Metastatic Castration-resistant Prostate Cancer AstraZeneca February 2017 Phase 3
NCT02789878 Not yet recruiting Prostate Cancer Instituto do Cancer do Estado de São Paulo|Janssen, LP February 2017 Phase 2
NCT02867020 Not yet recruiting Prostate Cancer Latin American Cooperative Oncology Group|Janssen Pharmaceuticals January 2017 Phase 2

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

P450 (e.g. CYP17)信号経路図

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID