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Description: Bimiralisib (also known as PQR-309; PI3K-IN-2) is an orally bioavailable, brain-penetrant, and balanced pan-inhibitor of PI3K/mTOR (phosphoinositide-3-kinase/mammalian target of rapamycin) with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kalpha, PI3Kdelta, PI3Kbeta, PI3Kgamma and mTOR, respectively. Bimiralisib has potential antineoplastic activity and is orally bioavailable, is able to cross the blood-brain barrier, and displayed favorable pharmacokinetic parameters in mice, rats, and dogs. Bimiralisib demonstrated efficiency in inhibiting proliferation in tumor cell lines and a rat xenograft model. Bimiralisib has a broad application range in oncology, including treatment of brain tumors or CNS metastasis. Bimiralisib is currently in phase II clinical trials for advanced solid tumors and refractory lymphoma.
References: J Med Chem. 2017 Sep 14; 60(17):7524-7538; Eur J Cancer. 2018 Jun; 96:6-16.
Related CAS#: 1820902-72-4 (HCl salt)' 1225037-39-7 (free base)
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