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  1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Abiraterone

Abiraterone  (Synonyms: 阿比特龍; CB-7598)

目錄號: HY-70013 純度: 99.88%
COA 產(chǎn)品使用指南

Abiraterone 是一種有效的不可逆的 CYP17A1 抑制劑,具有抗雄激素活性,抑制細胞色素 p450 酶 CYP17 的 17α-羥化酶和 17,20-裂合酶活性,IC50 值 分別為 2.5 nM 和 15 nM.

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Abiraterone Chemical Structure

Abiraterone Chemical Structure

CAS No. : 154229-19-3

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Customer Review

Other Forms of Abiraterone:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.

IC50 & Target

CYP17

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
35.8 nM
Compound: ABT
Inhibition of recombinant human CYP17 expressed in human A549 cell membranes using 17-alpha hydroxyprogesterone as substrate and NADPH as cofactor pretreated for 5 mins followed by substrate and cofactor addition after 60 mins by LC/MS analysis
Inhibition of recombinant human CYP17 expressed in human A549 cell membranes using 17-alpha hydroxyprogesterone as substrate and NADPH as cofactor pretreated for 5 mins followed by substrate and cofactor addition after 60 mins by LC/MS analysis
[PMID: 28350999]
A549 GI50
95 μM
Compound: Abiraterone
Antiproliferative activity against human A549 cells after 48 hrs by SRB assay
Antiproliferative activity against human A549 cells after 48 hrs by SRB assay
[PMID: 29172080]
DU-145 GI50
> 10 μM
Compound: abiraterone
Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 34908406]
ECa-109 cell line IC50
> 32 μM
Compound: Abiraterone
Antiproliferative activity against human EC109 cells after 72 hrs by MTT assay
Antiproliferative activity against human EC109 cells after 72 hrs by MTT assay
[PMID: 29310026]
GES1 IC50
13.12 μM
Compound: Abiraterone
Antiproliferative activity against human GES-1 cells after 72 hrs by MTT assay
Antiproliferative activity against human GES-1 cells after 72 hrs by MTT assay
[PMID: 29310026]
HBL-100 GI50
> 100 μM
Compound: Abiraterone
Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay
Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay
[PMID: 29172080]
HEK-293T IC50
> 100 μM
Compound: Abiraterone
Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36455509]
HeLa IC50
16.9 μM
Compound: Abiraterone
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36455509]
HeLa GI50
7.9 μM
Compound: Abiraterone
Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay
Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay
[PMID: 29172080]
HepG2 IC50
59.8 μM
Compound: Abiraterone
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36455509]
hTERT-BJ GI50
4.5 μM
Compound: Abiraterone
Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay
Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay
[PMID: 29172080]
LNCaP IC50
2706 nM
Compound: Abiraterone
Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay
Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay
[PMID: 36070471]
LNCaP IC50
3.29 μM
Compound: Abiraterone
Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay
Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay
[PMID: 29310026]
LNCaP IC50
800 nM
Compound: Abiraterone
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.
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.
[PMID: 12773039]
MCF7 IC50
19.3 μM
Compound: Abiraterone
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
[PMID: 27209562]
MCF7 IC50
38.2 μM
Compound: Abiraterone
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36455509]
MDA-MB-231 IC50
19.2 μM
Compound: Abiraterone
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 27209562]
MDA-MB-361 IC50
20.4 μM
Compound: Abiraterone
Growth inhibition of human MDA-MB-361 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-361 cells after 72 hrs by MTT assay
[PMID: 27209562]
MGC-803 IC50
7.72 μM
Compound: Abiraterone
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
[PMID: 29310026]
PC-3 GI50
> 10 μM
Compound: abiraterone
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 34908406]
PC-3 IC50
5.94 μM
Compound: Abiraterone
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
[PMID: 29310026]
PC-3 IC50
9.32 μM
Compound: Abiraterone
Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
[PMID: 24148837]
SK-OV-3 IC50
59.5 μM
Compound: Abiraterone
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36455509]
SW1573 GI50
85 μM
Compound: Abiraterone
Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay
Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay
[PMID: 29172080]
T47D IC50
16.9 μM
Compound: Abiraterone
Growth inhibition of human T47D cells after 72 hrs by MTT assay
Growth inhibition of human T47D cells after 72 hrs by MTT assay
[PMID: 27209562]
T47D GI50
24 μM
Compound: Abiraterone
Antiproliferative activity against human T47D cells after 48 hrs by SRB assay
Antiproliferative activity against human T47D cells after 48 hrs by SRB assay
[PMID: 29172080]
T47D IC50
34.7 μM
Compound: Abiraterone
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36455509]
WiDr GI50
42 μM
Compound: Abiraterone
Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay
Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay
[PMID: 29172080]
體外研究
(In Vitro)

已證實 Abiraterone 劑量 ≥5 μM 可顯著抑制 AR 陽性前列腺癌細胞系 LNCaP 和 VCaP 的增殖[2]。Abiraterone 對 17,20-裂解酶和 17α-羥化酶的 IC50 值分別為 15 nM 和 2.5 nM(CYP17 是一種具有 17α-羥化酶和 17,20-裂解酶活性的雙功能酶)。Abiraterone 抑制人類 17,20-裂解酶和 17α-羥化酶的 IC50 值分別為 27 和 30 nM[3]。Abiraterone 抑制重組人類 3βHSD1 和 3βHSD2 活性,競爭性 Ki 值分別為 2.1 和 8.8 μM。 10 μM Abiraterone 足以完全阻斷兩種細胞系中 5α-二酮和 DHT 的合成。使用 abi 治療可顯著抑制強勁增長亞群中的 CRPC 進展,有效地在 4 周的治療中限制腫瘤生長 (P<0.00001)。Abiraterone 可抑制 LNCaP 中的 [3H]-脫氫表雄酮 (DHEA) 耗竭和 Δ4-雄烯二酮 (AD) 積累,IC50 值 <1 μM[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

先前研究表明,0.5 mmol/kg/d Abiraterone 處理劑量可產(chǎn)生約 0.5 至 1 μM 的血清濃度。對照組異種移植腫瘤生長差異很大,一些腫瘤生長緩慢,只有一小部分腫瘤表現(xiàn)出強勁生長[4]。靜脈注射(5 mg/kg)后,清除率 (Cl) 和分布容積 (Vd) 值分別為 31.2 mL/min/kg 和 1.97 L/kg。AUC0-∞(從零時間點到無窮大時間點的血漿濃度-時間曲線下面積)值為 2675 ng*h/mL。終末半衰期 (t1/2) 值為 0.73 小時。由于清除率高,Abiraterone (ART) 僅在靜脈注射后 2 小時內(nèi)可量化[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

349.51

Formula

C24H31NO

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

阿比特龍;坦度酮羅;阿比特倫

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細胞實驗: 

Ethanol 中的溶解度 : 5 mg/mL (14.31 mM; 超聲助溶 (<60°C))

DMF 中的溶解度 : 5 mg/mL (14.31 mM; 超聲助溶 (<60°C))

DMSO 中的溶解度 : 2.5 mg/mL (7.15 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.8611 mL 14.3057 mL 28.6115 mL
5 mM 0.5722 mL 2.8611 mL 5.7223 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

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動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.88%

參考文獻
Cell Assay
[2]

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 (5 μM and 10 μM) at 24 and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4][5]

Mice[4]
Male NOD/SCID mice 6 to 8 weeks of age are surgically orchiectomized and implanted with a 5 mg 90-day sustained release DHEA pellet to mimic CRPC with human adrenal physiology. Two days later, 7×106 LAPC4 cells are injected subcutaneously with Matrigel. Tumor dimensions are measured 2 to 3 times per week, and volume is calculated as length×width×height×0.52. Once tumors reach 300 mm3, mice are randomly assigned to vehicle or Abiraterone treatment groups. Mice in the Abiraterone group are treated with 5 mL/kg intraperitoneal injections of 0.5 mmol/kg/d (0.1 mL 5% benzyl alcohol and 95% safflower oil solution) and control mice with vehicle only, once daily for 5 days per week over a duration of 4 weeks (n=8 mice per treatment). Statistical significance between Abiraterone and vehicle treatment groups is assessed by ANOVA based on a mixed-effect model.
Rats[5]
Male Sprague-Dawley rats (n=8, 240-260 g) are used. Blood samples (450 μL) are obtained following an i.v. 5 mg/kg dose of ART into polypropylene tubes containing Na2-EDTA solution as an anticoagulant and at pre-dose, 0.12, 0.25, 0.5, 1, 2, 4, 6, 8 and 24 h (a sparse sampling protocol is adopted during blood collection and at each time point blood is collected from four animals). Plasma is harvested by centrifuging the blood using a Biofuge at 1760g for 5 min and stored frozen at -80±10°C until analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol / DMF 1 mM 2.8611 mL 14.3057 mL 28.6115 mL 71.5287 mL
5 mM 0.5722 mL 2.8611 mL 5.7223 mL 14.3057 mL
Ethanol / DMF 10 mM 0.2861 mL 1.4306 mL 2.8611 mL 7.1529 mL
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產(chǎn)品名稱:
Abiraterone
目錄號:
HY-70013
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