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NVP-TNKS656

Cat. No. M3932
NVP-TNKS656 Structure
Synonym:

TNKS-656

Size Price Availability Quantity
10mM*1mL USD 229.5  USD255 In stock
2mg USD 94.5  USD105 In stock
5mg USD 207  USD230 In stock
10mg USD 360  USD400 In stock
25mg USD 648  USD720 In stock
50mg USD 1080  USD1200 In stock
100mg USD 1755  USD1950 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 494.58
Formula C27H34N4O5
CAS Number 1419949-20-4
Purity >98%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.
Shultz MD, et al. J Med Chem. 2013 Aug 22;56(16):6495-511. PMID: 23844574.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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