BAY1082439

SKU: orb1308580

Description

BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. It potently suppresses the growth of Pten-deficient prostate cancer and is also effective against tumors harboring PIK3CA mutations, as demonstrated in preclinical in vitro and in vivo studies.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1375469-38-7
• MW: 494.54
• Purity: 100.00% (May vary between batches)
• Formula: C₂₅H₃₀N₆O₅
• SMILES: COc1c(OC[C@H](O)CN2CCOCC2)ccc2C3=NCCN3C(NC(=O)c3cccnc3C)=Nc12
• Target: PI3K|||Apoptosis
• Solubility: DMSO:Slightly soluble

Bioactivity

• In Vivo:
  BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) effectively prevents the progression of Pten-null prostate cancer.
• In Vitro:
  BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells. BAY1082439 exhibits an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM) and shows >1000-fold selectivity against mTOR kinase.
  Read more...

Storage & Handling

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

Alternative Names

cancer, BAY1082439, BAY-1082439, BAY 1082439, Apoptosis, inhibit, mutated, oral, forms, Inhibitor, prostate, PTEN, Phosphoinositide 3-kinase, PI3K, PI3Kδ, PI3Kβ, PI3Kα, PIK3CA

Compound Identifiers

PubChem CID

135905473