| NVP-TNKS656TNKS2 inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 1419949-20-4 | SDF | Download SDF |
| Chemical Name | N-(cyclopropylmethyl)-N-((4-hydroxy-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)methyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)acetamide | ||
| Canonical SMILES | COC1=CC=C(C(C2CCN(CC(N(CC3=NC4=C(C(O)=N3)COCC4)CC5CC5)=O)CC2)=O)C=C1 | ||
| Formula | C27H34N4O5 | M.Wt | 494.58 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
NVP-TNKS656 is an orally active antagonist of Wnt pathway activity. The Wnt pathway has been involved in controlling numerous developmental processes. Dysfunction of this pathway may result in carcinogenesis [1].
In vitro: The IC50 value of NVP-TNKS656 against PARP1, TNKS2, PARP2, and STF was > 19, 0.006, 32, and 0.0035 µM, respectively [1].
In vivo: The clearance and volume of distribution of NVP-TNKS656 were 10 mL/min/kg and 0.6 L/kg after intravenous administration in mice. The exposure and oral bioavailability was 32% and 53%, respectively. In the mouse mammary tumor virus (MMTV)-Wnt1 transgenic model, oral administration of NVP-TNKS656 (350 mg/kg) activated the Wnt signaling over a 24-h time course. NVP-TNKS656 treatment reduced the Wnt/beta-catenintarget gene Axin2 mRNA level by 70-80% [1].
Reference:Shultz M D, Cheung A K, Kirby C A, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor[J]. Journal of medicinal chemistry, 2013, 56(16): 6495-6511.
