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ChemicalBook >> CAS DataBase List >>PX-866

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;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
Molecular Weight:
525.59
MDL Number:
MFCD11840616
MOL File:
502632-66-8.mol
Last updated:2023-06-08 09:02:11

PX-866 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
FDA UNII 987796874T

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302+H312+H332-H315-H319
Precautionary statements  P260-P280-P312
HS Code  29329990
NFPA 704
0
3 0

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
Product number Packaging Price Buy
13645 1mg $73 Buy
13645 5mg $306 Buy
13645 10mg $502 Buy
P840390 1mg $65 Buy
P840390 10mg $445 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

Global( 88)Suppliers
Supplier Tel Email Country ProdList Advantage
CONIER CHEM AND PHARMA LIMITED
+8618523575427 sales@conier.com China 49476 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32161 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
Hangzhou MolCore BioPharmatech Co.,Ltd.
+86-057181025280; +8617767106207 sales@molcore.com China 49734 58
Shanghai Acmec Biochemical Technology Co., Ltd.
+86-18621343501; +undefined18621343501 product@acmec-e.com China 33338 58
Aladdin Scientific
+1-+1(833)-552-7181 sales@aladdinsci.com United States 52924 58
SHANGHAI KEAN TECHNOLOGY CO., LTD.
+8613817748580 cooperation@kean-chem.com China 40066 58
Chemsky (shanghai) International Co.,Ltd 021-50135380 shchemsky@sina.com China 15402 60
BOC Sciences 1-631-485-4226; 16314854226 info@bocsci.com United States 14055 65
NCE Biomedical Co.,Ltd. 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 China 1493 55
(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 DJM-2-166 PX866;PX 866;DJM-166;DJM-2-166 QIUASFSNWYMDFS-NILGECQDSA-N 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
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