1375469-38-7
1375469-38-7 structure
- Name: BAY1082439
- Chemical Name: bay-1082439
- CAS Number: 1375469-38-7
- Molecular Formula: C25H30N6O5
- Molecular Weight: 494.543
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-02-15 03:24:54
- Modify Date: 2024-02-11 22:18:26
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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].
| Name | bay-1082439 |
|---|---|
| Synonyms |
bay-1082439
bay 2439 |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C25H30N6O5 |
| Molecular Weight | 494.543 |
| Exact Mass | 494.227783 |
| LogP | -0.20 |
| Index of Refraction | 1.683 |