| Identification | Back Directory | [Name]
BAY-1082439 | [CAS]
1375469-38-7 | [Synonyms]
CS-2422
BAY 2439
BAY-1082439
BAY-1082439; BAY 2439
BAY10-82439; BAY 10-82439; BAY-10-82439; BAY1082439; BAY 1082439; BAY-1082439
(R)-N-(8-(2-hydroxy-3-morpholinopropoxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylnicotinamide
N-[8-[[(2R)-2-Hydroxy-3-(morpholin-4-yl)propyl]oxy]-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-2-methylpyridine-3-carboxamide | [Molecular Formula]
C25H30N6O5 | [MDL Number]
MFCD31540439 | [MOL File]
1375469-38-7.mol | [Molecular Weight]
494.54 |
| Chemical Properties | Back Directory | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 5 mg/mL (10.11 mM; ultrasonic and adjust pH to 5 with HCl) | [form ]
A solid | [pka]
10.27±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
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| [IC 50]
PI3Kα; PI3Kβ; PI3Kδ | [References]
[1] Ningshu Liu, et al. Abstract 2799: BAY 1082439, a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN. Abstract nr 2799. doi:1538-7445.AM2012-2799.
[2] Yongkang Zou, et al. Co-Targeting the Cell Intrinsic and Microenvironment Pathways of Prostate Cancer by PI3Kα/β/δ inhibitor BAY1082439. Mol Cancer Ther. 2018 Oct;17(10):2091-2099. DOI:10.1158/1535-7163.MCT-18-0038 |
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