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938440-64-3

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Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014
The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency whilst maintaining or improving other key parameters, such as aqueous solubility and margins over hERG IC50, led to the discovery of the clinical candidate AZD8055 (14). Further optimization, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clinical candidate AZD2014 (21).
Pike, Kurt G.,Malagu, Karine,Hummersone, Marc G.,Menear, Keith A.,Duggan, Heather M.E.,Gomez, Sylvie,Martin, Niall M.B.,Ruston, Linette,Pass, Sarah L.,Pass, Martin
p. 1212 - 1216
(2013/03/14)

PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
There is provided compounds of formula (I), which are suitable for the treatment of cancer.
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Page/Page column 61-62

(2008/06/13)

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Chemical Properties

Boiling Point: 694.3 °C at 760 mmHg
Flash Point:373.7 °C
Density: 1.248 g/cm³
Solubility:DMSO: >2mg/mL (warmed)
Storage Temp.:Store at RT
Vapor Pressure: 3.09E-20mmHg at 25°C
Refractive Index: 1.609
PKA: 14.20±0.10(Predicted)
PSA: 93.07000
LogP: 2.77290

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