PX-866
- Product Name
- PX-866
- CAS No.
- 502632-66-8
- Chemical Name
- PX-866
- Synonyms
- PX-866;DJM-166;Sonolisib;DJM-2-166;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
- CBNumber
- CB1497362
- Molecular Formula
- C29H35NO8
- Formula Weight
- 525.59
- MOL File
- 502632-66-8.mol
PX-866 Property
- 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
Safety
- HS Code
- 29329990
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
N-Bromosuccinimide Price
- Product number
- 13645
- Product name
- PX 866
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 13645
- Product name
- PX 866
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $306
- Updated
- 2024/03/01
- Product number
- 13645
- Product name
- PX 866
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $502
- Updated
- 2024/03/01
- Product number
- P840390
- Product name
- PX-866
- Packaging
- 1mg
- Price
- $65
- Updated
- 2021/12/16
- Product number
- P840390
- Product name
- PX-866
- Packaging
- 10mg
- Price
- $445
- Updated
- 2021/12/16
PX-866 Chemical Properties,Usage,Production
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
Raw materials
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