xav-939

Synonym(s):3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one

CAS NO.：284028-89-3
Empirical Formula: C14H11F3N2OS
Molecular Weight: 312.31
MDL number: MFCD00106866
EINECS: 687-302-1
SAFETY DATA SHEET (SDS)
Update Date: 2026-02-02 18:10:39

What is xav-939?

Description

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

The Uses of xav-939

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.

The Uses of xav-939

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)

What are the applications of Application

XAV939 is a potent inhibitor of beta-catenin, TNKS1, and TNKS2

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.

Storage

Room temperature

References

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

Properties of xav-939

Boiling point:	429.3±55.0 °C(Predicted)
Density	1.5
Flash point:	213.4℃
storage temp.	room temp
solubility	DMSO: soluble5mg/mL, clear
form	powder
pka	0.23±0.20(Predicted)
color	white to beige
Stability:	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

Safety information for xav-939

Signal word	Danger
Pictogram(s)	Skull and Crossbones Acute Toxicity GHS06
GHS Hazard Statements	H301:Acute toxicity,oral H319:Serious eye damage/eye irritation
Precautionary Statement Codes	P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.