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BAY1082439

Chemical Structure : BAY1082439

CAS No.: 1375469-38-7

BAY1082439 (BAY10-82439, BAY 1082439)

Catalog No.: PC-63437Not For Human Use, Lab Use Only.

BAY1082439 is a potent, highly selective, orally available PI3Kα/β inhibitor with IC50 of 4.9 nM (PI3Kα), selectively inhibits both PI3Kα, including mutated forms of PIK3CA, and PI3Kβ in the PI3K/Akt/mTOR pathway.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BAY1082439 is a potent, highly selective, orally available PI3Kα/β inhibitor with IC50 of 4.9 nM (PI3Kα), selectively inhibits both PI3Kα, including mutated forms of PIK3CA, and PI3Kβ in the PI3K/Akt/mTOR pathway.
BAY1082439 displays >1000-fold selectivity against mTOR kinase.
BAY1082439 induces tumor cell apoptosis and growth inhibition in PI3K-expressing and/or PTEN-driven tumor cells.
BAY1082439 is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells.
BAY1082439 effectively inhibits Pten-null prostate cancer progression

Physicochemical Properties

M.Wt 494.228
Formula C25H30N6O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-(8-(2-hydroxy-3-morpholinopropoxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylnicotinamide

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. Mol Cancer Ther. 2018 Oct;17(10):2091-2099.

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