TAS-117

Names

[ Name ]:
TAS-117

[Synonym ]:
trans-3-Amino-1-methyl-3-[4-(3-phenylimidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]cyclobutanol
Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, trans-

Biological Activity

[Description]:

TAS-117 is a highly selective, non-ATP competitive pan-Akt inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively; shows minimal inhibitory activities against others kinases including PI3K, PDK1, and mTOR; inhibits Akt kinase activity but not p-Akt, blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1; induces significant cytotoxicity in MM cells associated with inhibition of IL6 secretion; triggers apoptosis and autophagy, induces ER stress response, inhibits human MM cell growth in murine xenograft models. Solid Tumors Phase 1 Clinical

[References]

References 1. Mimura N, et al. Cancer Res. 2014 Aug 15;74(16):4458-69. 2. Koji Ichikawa, et al. https://doi.org/10.1158/1535-7163.TARG-13-C177. View Related Products by Target Akt Solid Tumors

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
655.8±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₆H₂₄N₄O₂

[ Molecular Weight ]:
424.494

[ Flash Point ]:
350.4±34.3 °C

[ Exact Mass ]:
424.189911

[ LogP ]:
2.12

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.717

Related Compounds

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