Abiraterone Acetate

Modify Date: 2024-01-02 12:56:38

Abiraterone Acetate Structure
Abiraterone Acetate structure
 Common Name Abiraterone Acetate
CAS Number 154229-18-2 Molecular Weight 391.546
Density 1.1±0.1 g/cm3 Boiling Point 506.7±50.0 °C at 760 mmHg
Molecular Formula C26H33NO2 Melting Point 127-130°C
MSDS Chinese USA Flash Point 260.2±30.1 °C
Symbol GHS08
GHS08		 Signal Word Danger

 Use of Abiraterone Acetate


Abiraterone acetate is an oral, potent, selective, and irreversible inhibitor of CYP17.

 Names

Name abiraterone acetate
Synonym More Synonyms

 Abiraterone Acetate Biological Activity

Description Abiraterone acetate is an oral, potent, selective, and irreversible inhibitor of CYP17.
Related Catalog
Target

CYP17[1]
In Vitro Abiraterone (Abi) acetate is an ester prodrug of the anticancer agent Abiraterone, which 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[1]. 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 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 Abiraterone significantly inhibited CRPC progression in the robustly growing subset, effectively putting a ceiling on tumor growth over 4 weeks of treatment (P<0.00001)[3].
In Vivo Abiraterone (Abi) acetate prolongs survival in castration-resistant prostate cancer (CRPC). [3H]-dehydroepiandrosterone (DHEA) depletion and Δ4-androstenedione (AD) accumulation are inhibited by Abiraterone in LNCaP, with an IC50<1 μM. 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[3].
Cell Assay 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].
Animal Admin Mice[3] 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.
References

[1]. Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16(3):387-400.

[2]. Richards J, 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.

[3]. Li R, et al. Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clin Cancer Res. 2012 Jul 1;18(13):3571-9.

[4]. Lee GT, et al. Intracrine androgen biosynthesis in renal cell carcinoma. Br J Cancer. 2017 Mar 28;116(7):937-943.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 506.7±50.0 °C at 760 mmHg
Melting Point 127-130°C
Molecular Formula C26H33NO2
Molecular Weight 391.546
Flash Point 260.2±30.1 °C
Exact Mass 391.251129
PSA 39.19000
LogP 6.55
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.584
Storage condition -20°C Freezer

 Safety Information

Symbol GHS08
GHS08
Signal Word Danger
Hazard Statements H360-H372
Precautionary Statements P201-P260-P280-P308 + P313
Target Organs Endocrine system
Hazard Codes Xi
RIDADR NONH for all modes of transport
RTECS BV7992100
HS Code 2933399090

 Customs

HS Code 2933399090
Summary 2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles7

More Articles
Phase I clinical trial of the CYP17 inhibitor abiraterone acetate demonstrating clinical activity in patients with castration-resistant prostate cancer who received prior ketoconazole therapy.

J. Clin. Oncol. 28(9) , 1481-8, (2010)

Abiraterone acetate is a prodrug of abiraterone, a selective inhibitor of CYP17, the enzyme catalyst for two essential steps in androgen biosynthesis. In castration-resistant prostate cancers (CRPCs),...
Significant and sustained antitumor activity in post-docetaxel, castration-resistant prostate cancer with the CYP17 inhibitor abiraterone acetate.

J. Clin. Oncol. 28(9) , 1489-95, (2010)

The principal objective of this trial was to evaluate the antitumor activity of abiraterone acetate, an oral, specific, irreversible inhibitor of CYP17 in docetaxel-treated patients with castration-re...
Phase II multicenter study of abiraterone acetate plus prednisone therapy in patients with docetaxel-treated castration-resistant prostate cancer.

J. Clin. Oncol. 28(9) , 1496-501, (2010)

Persistence of ligand-mediated androgen receptor signaling has been documented in castration-resistant prostate cancers (CRPCs). Abiraterone acetate (AA) is a potent and selective inhibitor of CYP17, ...

 Synonyms

17-(3-pyridyl)-5,16-androstadien-3beta-acetate
Abiraterone acetate
Androsta-5,16-dien-3-ol, 17-(3-pyridinyl)-, acetate (ester), (3β)-
Zytiga
(3β)-17-(3-Pyridinyl)androsta-5,16-dien-3-yl acetate
(3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-yl acetate
Abiraterone (acetate)
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Related Compounds: More...
Abiraterone Acetate Dimer Impurity
186826-68-6
Abiraterone decanoate
2486052-18-8
Glutinol acetate
6426-44-4
Menthyl acetate
29066-34-0
chrysanthenyl acetate
54324-99-1
Germanicol acetate
10483-91-7
Cupric acetate monohydrate
6046-93-1
ethyl acetate, [1-14c]
27569-23-9
ethyl acetate-2-13C
58735-82-3
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