Epothilone A

Bezeichnung:Epothilone A

CAS-Nr152044-53-6

Englisch Name:Epothilone A

CBNumberCB6972280

SummenformelC26H39NO6S

Molgewicht493.66

MOL-Datei152044-53-6.mol

Epothilone A physikalisch-chemischer Eigenschaften

Schmelzpunkt	95℃
alpha	D21 -47.1° (c = 1.0 in methanol)
Siedepunkt	683.3±55.0 °C(Predicted)
Dichte	1.143
storage temp.	-20°C
Löslichkeit	Chloroform (Slightly), Ethyl Acetate (Slightly)
pka	13.57±0.70(Predicted)
Aggregatzustand	solid
Farbe	White to Off-White
Stabilität	Stable under recommended storage conditions., Stable Under Recommended Storage C
InChIKey	HESCAJZNRMSMJG-KKQRBIROSA-N
SMILES	[C@]12([H])[C@]([H])(O1)CCC[C@H](C)[C@H](O)[C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O[C@H](/C(/C)=C/C1=CSC(C)=N1)C2

Sicherheit

WGK Germany

Epothilone A Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
The epothilones are a novel class of antineoplastic agents possessing antitubulin activity. Epothilone A, B isolated from Sorangium cellulosum was associated with cell cycle arrest at G2/M transition and apoptosis that was resisted with overexpression of β-tubulin and P-glycoprotein in human bladder carcinoma cell.
Verwenden
Epothilone A is a microtubule inhibitor isolated from the myxobacteria, Sorangium cellulosum. Epothilone A acts by stabilising microtubule formation at the taxol binding site, and causes cell cycle arrest at the G2/M transition, leading to cytotoxicity. Epothilone A has been investigated in clinical trials as an antitumour agent.
Definition
ChEBI: An epithilone that is epothilone C in which the double bond in the macrocyclic lactone ring has been oxidised to the corresponding epoxide (the 13R,14S diastereoisomer).
Biologische Aktivität
epothilone a (epo a) is a naturally occurring microtubule-stabilizing macrolide that was first isolated from the myxobacterium sorangium cellulosum. the ic50 value of epothilone a in hct-116 cell line is 4.4 nm [1].it has been found that the skov-3 human ovarian cancer cells were susceptible to epothilone a with ic50 value of 20.4 ± 1.4 nm [2]. the antiproliferative capacity of epothilone a in skov-3 cell line (measured as ic50 after 72 h continuous treatment) was six times greater than that of ptx’s. besides, epothilone a induced time coursedependent apoptosis and necrosis [2].
target
MDR CCRF-CEM/VBL100 cells
Einzelnachweise
[1] regueiro-ren a1, borzilleri rm, zheng x, kim sh, johnson ja, fairchild cr, lee fy, long bh, vite gd. synthesis and biological activity of novel epothilone aziridines. org lett. 2001 aug 23;3(17):2693-6.
[2] rogalska a1, marczak a, gajek a, szwed m, śliwińska a, drzewoski j, jóźwiak z. induction of apoptosis in human ovarian cancer cells by new anticancer compounds, epothilone a and b. toxicol in vitro. 2013 feb;27(1):239-49.

Epothilone A Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

152044-53-6, Epothilone A Verwandte Suche:

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