| Identification | Back Directory | [Name]
NVP-TNKS656 | [CAS]
1419949-20-4 | [Synonyms]
TNKS656
CS-1333
NVP-TNKS656
NVP-TNKS656 - TNKS 656
TNKS656; TNKS-656;TNKS 656
1-Piperidineacetamide, N-(cyclopropylmethyl)-4-(4-methoxybenzoyl)-N-[(3,5,7,8-tetrahydro-4-oxo-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl]-
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
N-(cyclopropylmethyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)-N-((4-oxo-3,5,7,8-tetrahydro-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl)acetamide | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C27H34N4O5 | [MDL Number]
MFCD28167762 | [MOL File]
1419949-20-4.mol | [Molecular Weight]
494.58 |
| Chemical Properties | Back Directory | [Boiling point ]
700.7±70.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
Soluble in DMSO | [form ]
crystalline solid | [pka]
6.66±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Description]
NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM).1 It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/β-catenin target gene, in MMTV-Wnt1 tumor bearing mice. | [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]. | [References]
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. |
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Moltt Biocem Co., Ltd.
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