1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

NVP-TNKS656 (Synonyms: TNKS656)

Cat. No.: HY-13990 Purity: 99.14%
Data Sheet SDS 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

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $250 In-stock
2 mg $100 In-stock
5 mg $230 In-stock
10 mg $400 In-stock
25 mg $690 In-stock
50 mg $1200 In-stock
100 mg $1800 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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

IC50: 6 nM (TNKS2)

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].

References
Preparing Stock Solutions
Concentration Volume 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.
Animal Administration
[1]

NVP-TNKS656 is prepared in 4% HCl:10% propylene glycol:20% Solutol HS15:60.5% D5W:0.5% NaOH.

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
Molecular Weight

494.58

Formula

C₂₇H₃₄N₄O₅

CAS No.

1419949-20-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 40 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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