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Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor, Bimiralisib inhibits PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM, respectively. PQR309 also inhibits PI3Kα-H1047R, PI3Kα-E542K and PI3Kα-E545K with IC50s of 36 nM, 63 nM and 136 nM, respectively.
In vivo, both po and iv application routes show a rapid drop below 200 ng/mL (~0.5 μM) of PQR309 within <1 h (iv) to <2 h (po) after administration in mice, which reflects the time point when the compound reaches the median GI50 determined in tumor cell lines. In female rats a single oral dose (10 mg/kg) achieves similar drug levels as a single intravenous injection (5 mg/kg) with regard to Cmax.
| Molecular Weight | 411.38 |
| Formula | C17H20F3N7O2 |
| CAS Number | 1225037-39-7 |
| Solubility (25°C) | DMSO 21 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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