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WNTinib (APS-8-100-2), a multi-kinase inhibitor, selectively targets β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC) and impedes oncogenic Wnt signaling. It achieves this by inhibiting KIT/MAPK and subsequent activation of EZH2 [1].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | WNTinib (APS-8-100-2), a multi-kinase inhibitor, selectively targets β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC) and impedes oncogenic Wnt signaling. It achieves this by inhibiting KIT/MAPK and subsequent activation of EZH2 [1]. |
| In vitro | WNTinib induces apoptosis in CTNNB1 mutant models at 1μM over 3 days [1]. Additionally, WNTinib inhibits pEZH2 levels in HEPG2 cells at concentrations ranging from 0-30 μM for 1 hour [1]. In a Western Blot analysis of HEPG2 cells, a concentration of 0.5 μM after 24 hours of incubation resulted in inhibited levels of pT367 [1]. |
| In vivo | The half-life of WNTinib (20mg/kg;oral; 0-24 h) is 9.38 hours, with a plasma concentration of 7 μM 24 hours post-oral administration, and detectable amounts of the drug are present in plasma 72 hours after dosing [1]. Animal Model: mice [1]. Dosage: 20mg/kg. Administration: Tail vein injection; 5 days. Result: inhibited tumors. |
| Synonyms | APS-8-100-2 |
| Molecular Weight | 498.38 |
| Formula | C22H16F6N4O3 |
| Cas No. | 2770091-44-4 |
| Smiles | O(C=1C=C(C(NC)=O)N=CC1)C2=CC(F)=C(NC(NC3=CC=C(C(C(F)(F)F)(F)F)C=C3)=O)C=C2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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