| Bioactivity | Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively[1]. | ||||||||||||
| Invitro | Paxalisib (GDC-0084; Compound 16) maintains inhibition of each of the Class I PI3K isoforms but with more potent inhibition of mTOR. Paxalisib is also tested in five different GBM cell lines and is found to have antiproliferative EC50s ranging from 0.3 to 1.1 μM[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Paxalisib 相关抗体: | ||||||||||||
| In Vivo | After a 25 mg/kg dose of Paxalisib (GDC-0084; Compound 16) administered orally, pAKT in normal mouse brain tissue is significantly inhibited at 1 and 6 h postdose. The potent inhibition of pAKT at both time points in this study demonstrates that Paxalisib inhibits its target behind a fully intact BBB. In addition to the pharmacodynamic effect in normal brain tissue, Paxalisib is studied in a subcutaneous U87 tumor xenograft model of glioblastoma in mice. In this study, Paxalisib achieves significant and dose-dependent tumor growth inhibition. Tumor growth inhibition is first observed at a 2.2 mg/kg dose level. Higher doses led to greater tumor growth inhibition, including tumor regressions at the 17.9 mg/kg dose level. Each of these doses is well tolerated for the duration of the study[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
| CAS | 1382979-44-3 | ||||||||||||
| Formula | C18H22N8O2 | ||||||||||||
| Molar Mass | 382.42 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Heffron TP, et al. Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. |
Paxalisib
CAS: 1382979-44-3 F: C18H22N8O2 W: 382.42
Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for
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