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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 |
|---|
| 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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