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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product Name17-(3-pyridyl)-5,16-androstadien-3beta-acetate
SynonymsZYTIGA
CB 7630
Abirteroneacetate
Abiraterone Acetate
Abiraterone Acotate
Abiraterone Acetate impurity
17-(3-pyridyl)-5,16-androstadien-3beta-acetate

Synonyms

ZYTIGA
CB 7630
Abirteroneacetate
Abiraterone Acetate
Abiraterone Acotate
Abiraterone Acetate impurity
17-(3-pyridyl)-5,16-androstadien-3beta-acetate
(3β)-17-(3-pyridinyl) androsta-5,16-dien-3-yl acetate
(3)-17-(3-Pyridinyl)androsta-5,16-dien-3-ol Acetate (Ester)
(3beta,8xi,9xi,14xi)-17-(pyridin-3-yl)androsta-5,16-dien-3-yl acetate
[(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-pyridin-3-yl-2,3,4,7,8,9,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-3-yl] acetate
(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl acetate
CAS154229-18-2
EINECS620-314-7
Chemical FormulaC26H33NO2
Molecular Weight391.55
inchiInChI=1/C26H33NO2/c1-17(28)29-20-10-12-25(2)19(15-20)6-7-21-23-9-8-22(18-5-4-14-27-16-18)26(23,3)13-11-24(21)25/h4-6,8,14,16,20-21,23-24H,7,9-13,15H2,1-3H3/t20-,21?,23?,24?,25-,26+/m0/s1
Package10 mM * 1 mL;1 mg;5 mg;10 mg;50 mg;100 mg;500 mg
PriceEmail to quote
DescriptionsAbiraterone acetate

Abiraterone acetate

MedChemExpress (MCE)

HY-75054

154229-18-2

CB7630

99.96%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Room temperature in continental US

Descriptions

Abiraterone acetate

Abiraterone acetate

MedChemExpress (MCE)

HY-75054

154229-18-2

CB7630

99.96%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Room temperature in continental US
may vary elsewhere.

Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).

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[3].

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[3].

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.

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].

CYP17

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[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.
[Content Brief]

[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.
[Content Brief]

[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.
[Content Brief]

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

[5]. A O'Donnell, et al. Hormonal impact of the 17α-hydroxylase/C17,20-lyase inhibitor abiraterone acetate (CB7630) in patients with prostate cancer. British Journal of Cancervolume 90, pages2317–2325 (2004)

Supplier Websitehttps://www.medchemexpress.com/Abiraterone-acetate.html
Last Update2025-05-21 16:50:25
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