1. PI3K/Akt/mTOR
    Apoptosis
  2. PI3K
    Apoptosis
  3. BAY1082439

BAY1082439 

Cat. No.: HY-100886
Handling Instructions

BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.

For research use only. We do not sell to patients.

BAY1082439 Chemical Structure

BAY1082439 Chemical Structure

CAS No. : 1375469-38-7

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Description

BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth[1][2].

IC50 & Target[1]

PI3Kα

 

PI3Kβ

 

PI3Kδ

 

In Vitro

BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase[1].
BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells[2].

Cell Viability Assay[2]

Cell Line: PC3 and LNCaP cells (PTEN-null human prostate cancer cell lines)
Concentration: 0.1, 0.33, 1, 3.3, 10 μM
Incubation Time: 72 hours
Result: Efectively inhibited cell growth by blocking the G1/S cell cycle transition and by inducing apoptosis.
In Vivo

BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression[2].

Animal Model: Pten conditional knockout mouse model (Pb-Cre+;PtenL/L, CP model)[2]
Dosage: 75 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Significantly decreased tumor size and P-AKT staining, nearly normal luminal architecture, and a significant reduction of Ki67-positive cells. Significantly inhibit the human prostate cancer growth.
Molecular Weight

494.54

Formula

C₂₅H₃₀N₆O₅

CAS No.

1375469-38-7

SMILES

O=C(C1=CC=CN=C1C)NC2=NC3=C(C=CC(OC[[email protected]](O)CN4CCOCC4)=C3OC)C5=NCCN25

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BAY1082439BAY 1082439BAY-1082439PI3KApoptosisPhosphoinositide 3-kinaseoralmutatedformsPIK3CAloss-of-functionPTENprostatecancerInhibitorinhibitorinhibit

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BAY1082439
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