502632-66-8

502632-66-8 structure

Name: PX-866
Chemical Name: [(3aR,6E,9S,9aR,10R,11aS)-6-[[bis(prop-2-enyl)amino]methylidene]-5-hydroxy-9-(methoxymethyl)-9a,11a-dimethyl-1,4,7-trioxo-2,3,3a,9,10,11-hexahydroindeno[4,5-h]isochromen-10-yl] acetate
CAS Number: 502632-66-8
Molecular Formula: C₂₉H₃₅NO₈
Molecular Weight: 525.590
Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
Create Date: 2017-08-02 12:28:55
Modify Date: 2024-01-04 22:20:23
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].

Name	[(3aR,6E,9S,9aR,10R,11aS)-6-[[bis(prop-2-enyl)amino]methylidene]-5-hydroxy-9-(methoxymethyl)-9a,11a-dimethyl-1,4,7-trioxo-2,3,3a,9,10,11-hexahydroindeno[4,5-h]isochromen-10-yl] acetate
Synonyms	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

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