1419949-20-4
1419949-20-4 structure
- Name: NVP-TNKS656
- Chemical Name: nvp-tnks656
- CAS Number: 1419949-20-4
- Molecular Formula: C27H34N4O5
- Molecular Weight: 494.58300
- Catalog: Research Areas Cancer
- Create Date: 2018-12-25 16:32:37
- Modify Date: 2024-02-28 15:19:25
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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.
| Name | nvp-tnks656 |
|---|---|
| Synonyms | N-(cyclopropylmethyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)-N-((4-oxo-4,5,7,8-tetrahydro-3H-pyrano[4,3-d]pyrimidin-2-yl)methyl)acetamide |
| 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. |
|---|---|
| Related Catalog | |
| 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]. |
| Animal Admin | 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. |
| References |
| Molecular Formula | C27H34N4O5 |
|---|---|
| Molecular Weight | 494.58300 |
| Exact Mass | 494.25300 |
| PSA | 104.83000 |
| LogP | 2.12260 |
| Storage condition | -20℃ |