1. Cell Cycle/DNA Damage
    Apoptosis
    Epigenetics
  2. PARP
    Apoptosis
  3. NVP-TNKS656

NVP-TNKS656 (Synonyms: TNKS656)

Cat. No.: HY-13990 Purity: 99.31%
Handling Instructions

NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

For research use only. We do not sell to patients.

NVP-TNKS656 Chemical Structure

NVP-TNKS656 Chemical Structure

CAS No. : 1419949-20-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 300 In-stock
Estimated Time of Arrival: December 31
2 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 276 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 828 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2160 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

IC50 & Target

TNKS2

6 nM (IC50)

PARP2

32 μM (IC50)

In Vivo

NVP-TNKS656 (30 or 100 mg/kg, p.o.) exhibits good exposure and moderate oral bioavailability of 32% and 53%, respectively. Some slight overproportional increase in oral exposure is observed between 30 and 100 mg/kg with the dose normalized AUC for the 100 mg/kg dose being 2-fold higher than for the 30 mg/kg dose. Mice treated with NVP-TNKS656 (350 mg/kg, p.o.) show good plasma and tumor exposures corresponding to AUC0-24h of 515 and 325 μM·h, respectively[1].

Molecular Weight

494.58

Formula

C₂₇H₃₄N₄O₅

CAS No.

1419949-20-4

SMILES

O=C(N(CC1CC1)CC2=NC3=C(COCC3)C(N2)=O)CN4CCC(C(C5=CC=C(OC)C=C5)=O)CC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (80.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0219 mL 10.1096 mL 20.2192 mL
5 mM 0.4044 mL 2.0219 mL 4.0438 mL
10 mM 0.2022 mL 1.0110 mL 2.0219 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Athymic female nude mice weighing 19-22 g are implanted subcutaneously with a 3×3×3 mm3 tumor fragment from an MMTV-Wnt1 tumor-bearing mouse. Tumors are grown to approximately 250-300 mm3. Individual mice are given a single oral dose of vehicle (n=3) (4% HCl:10% propylene glycol:20% Solutol HS15:60.5% D5W:0.5% NaOH) or TNKS656 at 350 mg/kg (n=18). At 0.5, 1, 2, 4, 8, 16, or 24 h following dosing (n=3/time point), mice are euthanized, and blood is collected via cardiac puncture and processed for plasma. Tumors are excised from mice and frozen at −80°C for PD analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.31%

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Product name:
NVP-TNKS656
Cat. No.:
HY-13990
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