284028-89-3
xav-939
CAS: 284028-89-3
Molecular Formula: C14H11F3N2OS
284028-89-3 - Names and Identifiers
284028-89-3 - Physico-chemical Properties
| Molecular Formula | C14H11F3N2OS |
| Molar Mass | 312.31 |
| Density | 1.5 |
| Boling Point | 429.3±55.0 °C(Predicted) |
| Flash Point | 213.4℃ |
| Appearance | Shape powder, color white to beige |
| pKa | 0.23±0.20(Predicted) |
| Storage Condition | room temp |
| 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. |
| Physical and Chemical Properties | Bioactive XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription by inhibiting tankyrase1/2. IC50 is 11 nM/4 nM in cell-free test, which regulates axin level, but has no effect on CRE, NF-κB and TGF-β. |
| Use | Uses a tankyrase (TNKS) inhibitor that antagonizes Wnt signaling via stimulation of β-catenin degradation and stabilization of axin. XAV 939 inhibits proliferation of the Wei-catenin-dependent colon carcinom a cell line DLD-1. |
284028-89-3 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | R25 - Toxic if swallowed R36 - Irritating to the eyes |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S26/45 - |
| UN IDs | UN 2811 |
| WGK Germany | 3 |
| HS Code | 29349990 |
| Hazard Class | 6.1 |
| Packing Group | III |
284028-89-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.202 ml | 16.01 ml | 32.019 ml |
| 5 mM | 0.64 ml | 3.202 ml | 6.404 ml |
| 10 mM | 0.32 ml | 1.601 ml | 3.202 ml |
| 5 mM | 0.064 ml | 0.32 ml | 0.64 ml |
Last Update：2024-01-02 23:10:35
284028-89-3 - Uses and synthesis methods
Target
Target Value
TNKS2
(Cell-free assay) 4 nM
TNKS1
(Cell-free assay) 11 nM
in vitro studies
XAV939 is a small molecule selective inhibitor that inhibits transcription regulated by the Wnt pathway transcription factor β-catenin. The IC50 is 11 and 4nM when it acts on TNKS1 and TNKS2, respectively. XAV939 promotes the degradation of β-catenin by stabilizing the limit concentration composition of axin and the broken mixture, while stabilizing axin is by blocking the PAR enzyme: end anchor polymerase 1 and 2. The two end-anchor polymerase subtypes interact because of the highly conserved region of axin, which promotes the degradation of end-anchor polymerase through the ubiquitin-proteasome pathway. XAV939 inhibits Wnt/β-catenin pathway activity has been used in a variety of cancer treatments. XAV939 particularly inhibits end-anchor polymerase PARP activity. XAV939 significantly reduces the level of DNA-PKcs protein, indicating the key to end anchor polymerase PARP activity when maintaining the stability of DNA-PKcs protein. When treated with 1.0 μM XAV939 for 12 hours, the DNA-PKcs protein level was reduced to the lowest level. Compared with the control group treated with DMSO, the relative expression level was less than 25%. Treatment of human lymphocytes with 1.0 μM XAV939 resulted in a marked rise in end-anchor polymerase 1 levels.
In vivo studies
XAV-939 (3 mL, 10 nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model. XAV-939 (1 mg/mL, I .p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice.
Last Update：2024-04-09 21:01:54
Supplier List
Product Name: Baloxavir Impurity 121 Request for quotation
CAS: 284028-89-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 284028-89-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: XAV-939 Visit Supplier Webpage Request for quotationCAS: 284028-89-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: Baloxavir Impurity 121 Request for quotation
CAS: 284028-89-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 284028-89-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: XAV-939 Visit Supplier Webpage Request for quotationCAS: 284028-89-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History