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

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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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

494.54

Formula

C25H30N6O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (10.11 mM; ultrasonic and adjust pH to 5 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0221 mL 10.1104 mL 20.2208 mL
5 mM 0.4044 mL 2.0221 mL 4.0442 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0221 mL 10.1104 mL 20.2208 mL 50.5520 mL
5 mM 0.4044 mL 2.0221 mL 4.0442 mL 10.1104 mL
10 mM 0.2022 mL 1.0110 mL 2.0221 mL 5.0552 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BAY1082439
Cat. No.:
HY-100886
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