Abiraterone Acetate (CB 7630) is a highly active and selective 17α-hydroxylase/17,20 lyase (CYP17A1) inhibitor with an IC50 of 72 nM. Abiraterone Acetate (CB 7630) inhibitor CYP11B1, CYP11B2 and CYP3A4 with IC50 of 1.6, 1.8 and 2.7 μM. Abiraterone Acetate (CB 7630) is used in the study of castration-resistant prostate cancer. Abiraterone Acetate (CB 7630) blocks the formation of testosterone by inhibiting CYP17A1. Abiraterone Acetate (CB 7630) caused significant reductions in the weights of the ventral prostate and seminal vesicles. There was no reduction seen in the weight of these organs with KC. Abiraterone Acetate (CB 7630) reduced plasma testosterone to 0.1 nM or less, despite a three- to four-fold increase in the plasma level of luteinizing hormone (LH).
|Cell lines||LNCaP and VCaP cells|
|Preparation method||Seeding LNCaP and VCaP cells in 96-well plates and growing in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days.Treatig cells with Abiraterone at 24 hours and 96 hours after plating and determining cell viability on day 7 by adding CellTiter Glo and measuring luminescence|
|Concentrations||0 μM -10 μM|
|Incubation time||24 hours and 96 hours|
|Animal models||Male NOD/SCID mice with LAPC4 cells|
|Formulation||0.1 mL 5% benzyl alcohol and 95% safflower oil solution|
|Administration||Administered via s.c.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||Ethanol 20 mg/mL|
|Related Cytochrome P450 (e.g. CYP17) Products|
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.
ε-Viniferin is a potent inhibitor for all the CYP family, with Ki values from 0.5-20 μM.
Rhapontigenin is a selective inactivator of cytochrome P450 1A1 with IC50 of 400 nM.
(Rac)-Brassinazole is a brassinosteroid (BR) biosynthesis inhibitor.
Stiripentol is an LDH inhibitor.
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