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| Product Name: | PX-866 | | Synonyms: | (1E,4S,4aR,5R,6aS,9aR)-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-cyclopenta[5,6]naphtho[1,2-c]pyran-2,7,10(1H)-trione;(2R,3S,6Z,11R,15S,17R)-6-{[bis(prop-2-en-1-yl)aMino]Methylidene}-8-hydroxy-3-(MethoxyMethyl)-2,15-diMethyl-5,9,14-trioxo-4-oxatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1(10),7-dien-17-yl acetate;Sonolisib;(2R,3S,6Z,11R,15S,17R)-6-{[bis(prop-2-en-1-yl)aMino]Methylidene}-8-hydroxy-3-(MethoxyMethyl)-2,15-diMethyl-5,9,14-trioxo-4-oxatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1(10),7-dien-17-yl;PX-866;Acetic acid (1S,4E,10R,11R,13S,14R)-[4-diallylaminomethylene-6-hydroxy-1-methoxymethyl-10,13-dimethyl-3,7,17-trioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester;PX-866 (Sonolisib);DJM-166 | | CAS: | 502632-66-8 | | MF: | C29H35NO8 | | MW: | 525.59 | | EINECS: | | | Product Categories: | | | Mol File: | 502632-66-8.mol |  |
| | PX-866 Chemical Properties |
| Boiling point | 651.4±55.0 °C(Predicted) | | density | 1.28 | | storage temp. | 2-8°C | | solubility | Soluble in DMSO (up to 25 mg/ml). | | form | solid | | pka | 8.35±0.70(Predicted) | | color | Orange | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. | | CAS DataBase Reference | 502632-66-8 |
| | PX-866 Usage And Synthesis |
| Description | PX-866 (502632-66-8) inhibits PI-3 Kinase with selectivity for p110α (IC50=0.1 nM). Counteracts hypoxia-related downregulation of E7 expression in HPV-positive cancer cells.2 Displays antitumor activity. Irreversible. Cell permeable. | | Uses | PX-866 is an analog of wortmannin (W499400). Wortmannin is a phosphatidylinositol 3 kinase (PI3K) inhibitor. Potent PI3K inhibitor. | | Definition | ChEBI: PX-866 is an organic heterotetracyclic compound that is obtained from wortmanin via aminolysis of its furan ring by diallyl amine. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor. It is an organic heterotetracyclic compound, a delta-lactone, an acetate ester and a tertiary amino compound. It is functionally related to a wortmannin. | | in vitro | in previous study, px 866 was identified to be able to inhibit purified ptdins-3-kinase and ptdins-3-kinase signaling that was measured by phospho-ser473-akt levels in ht-29 colon cancer cells [1]. | | in vivo | animal study found that px-866 treatment at 10 mg/kg to mice could inhibit phospho-ser473-akt in ht-29 colon tumor xenografts up to 80% with recovery taking over 48 hours after oral administration but more rapidly after iv or ip route. in addition, px-866 had in-vivo antitumor activity against s.c. ovcar-3 human ovarian cancer and a-549 human lung cancer xenografts in immunodeficient mice. moreove, px-866 could also increase the antitumor activity of cisplatin against a-549 xenografts and radiation treatment against ovcar-3 xenografts [1]. | | Enzyme inhibitor | This orally active antifungal and antineoplastic agent (FW = 541.60 g/mol; CAS 502632-66-8; Solubility: 40 mg/mL DMSO, water-insoluble; stable for six months, when stored in a refrigerated desicator) is a chemically stable wortmannin derivative that potently and irreversibly inhibits phosphoinositide 3-kinase (IC50 = 0.1 nM) and phosphoinositide-3-kinasedependent signaling. PX-866 blocks PtdIns-3-kinase signaling, as measured by phospho-Ser473-Akt levels in HT-29 colon cancer cells (IC50 = 20 nM). PX-866 also overcomes resistance to the EGFR inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. | | IC 50 | 0.1-88 nm | | References | 1) Ihle et al. (2004), Molecular pharmacology and antitumor activity of PK-866, a novel inhibitor of phosphoinositide-3-kinase signaling; Mol. Cancer Ther., 3 763
2) Bossler et al. (2019) Repression of Human Papilloma Virus Oncogene Expression Under Hypoxia is Mediated by PI3K/mTORC2/AKT Signaling; mBio,?10 e02323 [Focus Citation] |
| | PX-866 Preparation Products And Raw materials |
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