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BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2]. Additionally, BAY1082439 is effective against mutated forms of PIK3CA.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
2 mg | $44 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $122 | In Stock | |
25 mg | $198 | In Stock | |
50 mg | $369 | In Stock | |
100 mg | $549 | In Stock |
Description | BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2]. Additionally, BAY1082439 is effective against mutated forms of PIK3CA. |
In vitro | BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. 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]. BAY1082439 exhibits an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM) and shows >1000-fold selectivity against mTOR kinase[1]. |
In vivo | BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) effectively prevents the progression of Pten-null prostate cancer[2]. |
Molecular Weight | 494.54 |
Formula | C25H30N6O5 |
Cas No. | 1375469-38-7 |
Smiles | COc1c(OC[C@H](O)CN2CCOCC2)ccc2C3=NCCN3C(NC(=O)c3cccnc3C)=Nc12 |
Relative Density. | 1.43 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO: Slightly soluble |
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