Abiraterone

SKU: orb1300971

Description

Abiraterone

Research Area

Metabolism Research

Key Properties

• CAS Number: 154229-19-3
• MW: 349.509
• Purity: 99.93% (May vary between batches)
• Formula: C₂₄H₃₁NO
• SMILES: C[C@]12CC[C@H]3[C@@H](CC=C4C[C@@H](O)CC[C@]34C)[C@@H]1CC=C2C1=CN=CC=C1
• Target: Cytochromes P450
• Solubility: Ethanol:7.21 mg/mL (20.63 mM);DMF:8.75 mg/mL (25.04 mM);DMSO:0.87 mg/mL (2.49 mM)

Bioactivity

• Target IC50:
  CYP17:2 nM
• In Vivo:
  Abiraterone inhibits the proliferation in vitro and the androgen receptor-mediated gene expression in androgen receptor-positive prostate cancer cells, likely through the suppression of steroidogenesis and anti-androgen receptor activity. At higher concentrations, Abiraterone inhibits the activation of mutant androgen receptors by enzalutamide. Abiraterone effectively replaces the ligand in WT-AR (EC50: 13.4 μM) and T877A mutant receptors (EC50: 7.9 μM). Additionally, Abiraterone acetate significantly suppresses testosterone secretion by 48% and increases LH levels to 192%. Abiraterone also inhibits the lysosomal activity in rat testicular microsomes (IC50: 5.8 nM).
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• In Vitro:
  Abiraterone effectively reduces testosterone levels almost to the extent of testicular removal without significantly decreasing the size of any organ. It inhibits CYP17 in human testicular microsomes (IC50: 72 nM), leading to a reduction in testosterone levels by over 95% compared to the control group.
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• Cell Research:
  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 at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CYP17, CYPs, Cytochrome P450, CB 7598, CB7598, CB-7598, Abiraterone, Inhibitor, inhibit

Compound Identifiers

PubChem CID

132971