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PX-866

Names

[ CAS No. ]:
502632-66-8

[ Name ]:
PX-866

[Synonym ]:
Cyclopenta[5,6]naphtho[1,2-c]pyran-2,7,10(1H)-trione, 5-(acetyloxy)-1-[(di-2-propen-1-ylamino)methylene]-4,4a,5,6,6a,8,9,9a-octahydro-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-, (1E,4S,4aR,5R,6aS,9aR)-
PX-866
(1E,4S,4aR,5R,6aS,9aR)-1-[(diprop-2-en-1-ylamino)methylidene]-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,7,10-trioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate
DJM-2-166
(1E,4S,4aR,5R,6aS,9aR)-1-[(Diallylamino)methylene]-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,7,10-trioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate
DJM-166
Sonolisib

Biological Activity

[Description]:

Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

[Target]

p110α:0.1 nM (IC50)

p110δ:2.9 nM (IC50)

p120γ:1 nM (IC50)


[In Vitro]

Sonolisib (PX-866) inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations[3].

[References]

[1]. Ihle NT, et al. The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growthfactor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. Mol Cancer Ther. 2005 Sep;4(9):1349-57.

[2]. Bowles DW, et al. A Randomized, Phase II Trial of Cetuximab With or Without PX-866, an Irreversible Oral Phosphatidylinositol 3-Kinase Inhibitor, in Patients With Metastatic Colorectal Carcinoma. Clin Colorectal Cancer. 2016 Dec;15(4):337-344.e2.

[3]. Sonolisib

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
651.4±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C29H35NO8

[ Molecular Weight ]:
525.590

[ Flash Point ]:
347.7±31.5 °C

[ Exact Mass ]:
525.236267

[ PSA ]:
119.44000

[ LogP ]:
2.37

[ Vapour Pressure ]:
0.0±4.4 mmHg at 25°C

[ Index of Refraction ]:
1.586

Related Compounds