PX-866
- CAS No.
- 502632-66-8
- Chemical Name:
- PX-866
- 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
- CBNumber:
- CB1497362
- Molecular Formula:
- C29H35NO8
- Molecular Weight:
- 525.59
- MDL Number:
- MFCD11840616
- MOL File:
- 502632-66-8.mol
| 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 |
| FDA UNII | 987796874T |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302+H312+H332-H315-H319 | |||||||||
| Precautionary statements | P260-P280-P312 | |||||||||
| HS Code | 29329990 | |||||||||
| NFPA 704 |
|
PX-866 price More Price(16)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 13645 | PX 866 ≥98% | 502632-66-8 | 1mg | $73 | 2024-03-01 | Buy |
| Cayman Chemical | 13645 | PX 866 ≥98% | 502632-66-8 | 5mg | $306 | 2024-03-01 | Buy |
| Cayman Chemical | 13645 | PX 866 ≥98% | 502632-66-8 | 10mg | $502 | 2024-03-01 | Buy |
| TRC | P840390 | PX-866 | 502632-66-8 | 1mg | $65 | 2021-12-16 | Buy |
| TRC | P840390 | PX-866 | 502632-66-8 | 10mg | $445 | 2021-12-16 | Buy |
PX-866 Chemical Properties,Uses,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
Preparation Products
PX-866 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +undefined18621343501 | product@acmec-e.com | China | 33349 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Chemsky (shanghai) International Co.,Ltd | 021-50135380 | shchemsky@sina.com | China | 15421 | 60 |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 14059 | 65 |
| NCE Biomedical Co.,Ltd. | 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 | China | 1494 | 55 | |
| AdooQ BioScience, LLC | +1 (866) 930-6790 | info@adooq.com | United States | 2784 | 58 |