| Identification | Back Directory | [Name]
PX-866 | [CAS]
502632-66-8 | [Synonyms]
PX-866
DJM-166
DJM-2-166
Sonolisib
Sonolisib (PX866)
PX-866 (Sonolisib)
QIUASFSNWYMDFS-NILGECQDSA-N
PX866;PX 866;DJM-166;DJM-2-166
(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
(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
(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
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)-
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 | [Molecular Formula]
C29H35NO8 | [MDL Number]
MFCD07784511 | [MOL File]
502632-66-8.mol | [Molecular Weight]
525.59 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]. | [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-kinase-
dependent 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. | [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]. | [IC 50]
0.1-88 nm | [storage]
Store at -20°C | [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] |
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BOC Sciences
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