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;PX-866, PI3-kinase inhibitor;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
CBNumber: CB1497362
Molecular Formula: C29H35NO8
Formula Weight: 525.59
MOL File: 502632-66-8.mol

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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

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Safety

HS Code: 29329990

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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.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 13645
Product name: PX 866
Purity: ≥98%
Packaging: 1mg
Price: $73
Updated: 2024/03/01

Cayman Chemical

Product number: 13645
Product name: PX 866
Purity: ≥98%
Packaging: 5mg
Price: $306
Updated: 2024/03/01

Cayman Chemical

Product number: 13645
Product name: PX 866
Purity: ≥98%
Packaging: 10mg
Price: $502
Updated: 2024/03/01

TRC

Product number: P840390
Product name: PX-866
Packaging: 1mg
Price: $65
Updated: 2021/12/16

TRC

Product number: P840390
Product name: PX-866
Packaging: 10mg
Price: $445
Updated: 2021/12/16

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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

Preparation Products

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PX-866 Suppliers

China 72 Switzerland 1 United Kingdom 2 United States 15 Global 90

BOC Sciences

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502632-66-8, PX-866Related Search:

Ko 143 CYCLOPAMINE Imatinib mesylate (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT

PX-866 (Sonolisib)

DJM-166

DJM-2-166

PX866;PX 866;DJM-166;DJM-2-166

(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

QIUASFSNWYMDFS-NILGECQDSA-N

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

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)-

Sonolisib (PX866)

PX-866, PI3-kinase inhibitor

502632-66-8