xav-939

Bezeichnung:xav-939

CAS-Nr284028-89-3

Englisch Name:xav-939

CBNumberCB82501008

SummenformelC14H11F3N2OS

Molgewicht312.31

MOL-Datei284028-89-3.mol

xav-939 physikalisch-chemischer Eigenschaften

Siedepunkt	429.3±55.0 °C(Predicted)
Dichte	1.5
Flammpunkt	213.4℃
storage temp.	room temp
Löslichkeit	DMSO: soluble5mg/mL, clear
Aggregatzustand	powder
pka	0.23±0.20(Predicted)
Farbe	white to beige
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25-36
S-Sätze:	26-45-26/45
RIDADR	UN 2811
WGK Germany	3
HazardClass	6.1
PackingGroup	III
HS Code	29349990

Gefahreninformationscode (GHS)

xav-939 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
XAV-939 (284028-89-3) is a tankyrase inhibitor (IC50=11 and 4 nM for TNKS1 and 2 respectively).? Antagonizes wnt signaling via stimulation of β-catenin degradation and stabilization of actin.1? XAV-939 robustly induces cardiomyogenesis of stem cells.2? Cell permeable
Verwenden
A tankyrase (TNKS) inhibitor that antagonizes Wnt signaling via stimulation of β-catenin degradation and stabilization of axin. It inhibits proliferation of the μ-catenin-dependent colon carcinoma cell line DLD-1.
Verwenden
XAV939 has been used in the inhibition
- of tankyrase in neuroblastoma cell lines
- of diphtheria toxin-like ADP-ribosyltransferases (ARTD) in medulloblastoma cells
- of wnt signalling in human induced pluripotent stem cells (hiPSCs)
Definition
ChEBI: XAV939 is a thiopyranopyrimidine in which a 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine skeleton is substituted at C-4 by a hydroxy group and at C-2 by a para-(trifluoromethyl)phenyl group. It has a role as a tankyrase inhibitor. It is a thiopyranopyrimidine and a member of (trifluoromethyl)benzenes.
Biochem/physiol Actions
XAV939 is a cell-permeable dihydrothiopyranopyrimidinol, which elicits anti-tumor functionality against colon, lung, breast and liver cancer. It binds to catalytic poly-ADP-ribose polymerase (PARP) domain of the tankyrase enzyme resulting in β-catenin destruction. It also inhibits tankyrase in neuroblastoma promoting apoptosis in tumor cells.
Lager
Room temperature
Einzelnachweise
1) Huang?et al. (2009),?Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling; Nature,?46?614 2) Wang?et al. (2011),?Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling; Chem. Biol.,?6?192

xav-939 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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