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NVP-TNKS656

Cat. No. M3932

All AbMole products are for research use only, cannot be used for human consumption.

NVP-TNKS656 Structure
Synonym:

TNKS-656

Size Price Availability Quantity
10mM*1mL in DMSO USD 88  USD88 In stock
2mg USD 50  USD50 In stock
5mg USD 85  USD85 In stock
10mg USD 135  USD135 In stock
25mg USD 270  USD270 In stock
50mg USD 430  USD430 In stock
100mg USD 620  USD620 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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
Protocol (for reference only)
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.
Chemical Information
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
References

[1] Shultz MD, et al. J Med Chem. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.

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Keywords: NVP-TNKS656, TNKS-656 supplier, PARP, inhibitors, activators

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