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BAY1082439 is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha and beta isoforms with potential antineoplastic activity. BAY 1082439 showed clear advantages over the strong PI3Kα inhibitor BAY 80-6946 in PTEN/PI3Kα-driven tumor models (e.g., PC3 and HEC-1B), when the two compounds were compared at their MTDs. Furthermore, BAY 1082439 has unique pharmacokinetic (PK) properties with very high plasma free fractions across all species tested (33-50%), large Vss, high clearance and intermediate T1/2.
With once daily dosing, BAY 1082439 could induce tumor regression in KPL4 (PIK3CAmut and HER2+), and tumor stasis in HEC-1B (PTENdel) and in HEC-1A (PIK3CAmut) tumor models.
| Molecular Weight | 494.54 |
| Formula | C25H30N6O5 |
| CAS Number | 1375469-38-7 |
| Solubility (25°C) | DMSO 10 mM (ultrasonic and adjust pH to 5 with HCl) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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