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Bimiralisib

CAS No. : 1225037-39-7

MCE 站：Bimiralisib

产品活性：Bimiralisib (PQR309) 是一种有效的，可渗透脑的，PI3K/mTOR 抑制剂，抑制 PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ 和 mTOR，IC₅₀ 分别为 33 nM，451 nM，661 nM，708 nM 和 89 nM。Bimiralisib 是 mTORC1 和 mTORC2 抑制剂。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K  |  mTOR

In Vitro: Bimiralisib is a highly selective pan-PI3K inhibitor with a balanced targeting of mTOR kinase. Bimiralisib also inhibits PI3Kα-H1047R), PI3Kα-E542K and PI3Kα-E545K with IC₅₀s of 36 nM, 63nM and 136 nM, respectively.

In Vivo: Oral administration yields similar concentrations of Bimiralisib in brain and plasma samples illustrates that Bimiralisib readily passes the blood–brain barrier. In mice, 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, which reflects the time point when the drug 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 C_max. The half-life of 5-8 h and an AUC_0.25-12 of around 14 000 h?ng/mL contributed to an excellent oral bioavailability of PQR309 (>50%). Twenty-four hours after po administration, plasma levels of PQR309 are still >2 μM (800-1000 ng/mL). Moreover, after 1-2 h exposure to PQR309 , drug levels in rat brain samples are comparable to plasma levels, confirming rapid access of PQR309 to the brain.

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