XAV-939 inhibits tankyrases and wnt pathway signaling. XAV exhibits anti-fibrotic activity and shows potential anticancer chemotherapeutic benefit when co-administered with other compounds. XAV-939 decreases nuclear accumulation of β-catenin and decreases c-myc levels, decreasing bleomycin-induced dermal thickening. In both in vitro and in vivo models of cancer, this compound reverses resistance to PI3K and Akt inhibitors.
| Cas No. | 284028-89-3 |
|---|---|
| Purity | ≥95% |
| Formula | C14H11F3N2OS |
| Formula Wt. | 312.31 |
| Chemical Name | 2-[4-(trifluoromethyl)phenyl]-7,8-dihydro-5H-thiino[4,3-d]pyrimidin-4-ol |
| IUPAC Name | 2-[4-(Trifluoromethyl)phenyl]-1,5,7,8-tetrahydro-4H-thiopyrano[4,3-d]pyrimidin-4-one |
| Solubility | DMSO (25mg/ml) |
| Appearance | White to off white powder |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| Info Sheet | X0384 Info Sheet PDF |
|---|
Bilir B, Kucuk O, Moreno CS. Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells. J Transl Med. 2013 Nov 4;11(1):280. [Epub ahead of print]. PMID: 24188694
Distler A, Deloch L, Huang J, et al. Inactivation of tankyrases reduces experimental fibrosis by inhibiting canonical Wnt signalling. Ann Rheum Dis. 2013 Sep 1;72(9):1575-80. PMID: 23148305.
Tenbaum SP, Ordóñez-Morán P, Puig I, et al. β-catenin confers resistance to PI3K and AKT inhibitors and subverts FOXO3a to promote metastasis in colon cancer. Nat Med. 2012 Jun;18(6):892-901. PMID: 22610277.
