NVP-TNKS656(TNKS-656) is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; >300 fold selectivity against PARP1 and PARP2. NVP-TNKS656 was identified as an orally active antagonist of Wnt pathway activity in the MMTV-Wnt1 mouse xenograft model. With an enthalpy-driven thermodynamic signature of binding, highly favorable physicochemical properties, and high lipophilic efficiency, NVP-TNKS656 is well suited for further in vivo validation studies.
Ann N Y Acad Sci. 2019 May;1443(1):54-74.
The Wnt signaling pathway: a potential therapeutic target against cancer.
NVP-TNKS656 purchased from AbMole
Cancer Treat Rev. 2017 Nov 3;50–60.
Targeting the Wnt/beta-catenin Pathway in Cancer: Update on Effectors and Inhibitors
NVP-TNKS656 purchased from AbMole
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Source | Clin Cancer Res (2016). Figure 4. NVP-TNKS656 |
| Method | Apoptosis assays | |
| Cell Lines | colorectal cancer cell lines | |
| Concentrations | 100 nmol/L | |
| Incubation Time | 48 hours | |
| Results | The repression of the Wnt/b-catenin pathway by NVP-TNKS656 alone did not promote apoptosis in DLD1 or HT29 colon cancer cells but enhanced the apoptosis induced by exogenous nuclear FOXO3A-ER |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Athymic female nude mice bearing MMTV-Wnt1 tumors |
| Formulation | 4% HCl:10% propylene glycol:20% Solutol HS15:60.5% D5W:0.5% NaOH |
| Dosages | 350 mg/kg |
| Administration | p.o. |
| Molecular Weight | 494.58 |
| Formula | C27H34N4O5 |
| CAS Number | 1419949-20-4 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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