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

Abiraterone (Synonyms: CB-7598)

製品番号: HY-70013 純度: 99.61%
取扱説明書

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.

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Abiraterone 構造式

Abiraterone 構造式

CAS 番号 : 154229-19-3

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMF USD 66 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 60 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 74 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 96 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 144 在庫あり
Estimated Time of Arrival: December 31
1 g USD 180 在庫あり
Estimated Time of Arrival: December 31
2 g USD 288 在庫あり
Estimated Time of Arrival: December 31
5 g USD 528 在庫あり
Estimated Time of Arrival: December 31
10 g   お問い合わせ  
50 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Abiraterone:

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製品説明

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

IC50:17α-hydroxylase (2.5 nM), 17,20-lyase (15 nM)[6]

体外実験

Significant inhibition of proliferation of the AR-positive prostate cancer cell lines LNCaP and VCaP with doses of Abiraterone ≥5 μM is confirmed[2]. Abiraterone shows IC50 values of 15 nM and 2.5 nM for the 17,20-lyase and 17α-hydroxylase (CYP17 is a bifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activity). Abiraterone inhibits human 17,20-lyase and 17α-hydroxylase with IC50 of 27 and 30 nM respectively[3]. Abiraterone inhibits recombinant human 3βHSD1 and 3βHSD2 activity with competitive Ki values of 2.1 and 8.8 μM. 10 μM Abiraterone is sufficient to completely block synthesis of 5α-dione and DHT in both cell lines.Treatment with abi significantly inhibited CRPC progression in the robustly growing subset, effectively putting a ceiling on tumor growth over 4 weeks of treatment (P<0.00001). [3H]-dehydroepiandrosterone (DHEA) depletion and Δ4-androstenedione (AD) accumulation are inhibited by Abiraterone in LNCaP, with an IC50<1 μM[4].

体内実験

The 0.5 mmol/kg/d Abiraterone treatment dose is previously shown to yield serum concentrations of about 0.5 to 1 μM. Xenograft tumor growth in the control group is widely variable, with some tumors growing slowly and only a subset of tumors exhibiting robust growth[4]. Following i.v. administration (5 mg/kg) the clearance (Cl) and volume of distribution (Vd) are found to be 31.2 mL/min/kg and 1.97 L/kg, respectively. The AUC0-∞ (area under the plasma concentration-time curve from time zero to infinity time point) is found to be 2675 ng*h/mL. The terminal half-life (t1/2) is 0.73 h. Because of high clearance, Abiraterone (ART) is quantifiable only until 2 h following i.v. administration[5].

臨床実験
分子量

349.51

分子式

C₂₄H₃₁NO

CAS 番号

154229-19-3

SMILES

C[[email protected]@]12C(C3=CN=CC=C3)=CC[[email protected]]1([[email protected]@]4(CC=C5[[email protected]@](C)([[email protected]]4(CC2)[H])CC[[email protected]@H](C5)O)[H])[H]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMF : 8.75 mg/mL (25.04 mM; Need ultrasonic and warming)

Ethanol : 5.4 mg/mL (15.45 mM; Need ultrasonic)

DMSO : 5 mg/mL (14.31 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2861 mL 1.4306 mL 2.8611 mL
*Please refer to the solubility information to select the appropriate solvent.
参考文献
細胞実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 99.61%

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Keywords:

AbirateroneCB-7598CB7598CB 7598Cytochrome P450CYPsInhibitorinhibitorinhibit

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製品名:
Abiraterone
製品番号:
HY-70013
数量:
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