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NVP-TNKS656

NVP-TNKS656 Structure
NVP-TNKS656
  • CAS No.1419949-20-4
  • Chemical Name:NVP-TNKS656
  • CBNumber:CB42705091
  • Molecular Formula:C27H34N4O5
  • Formula Weight:494.58
  • MOL File:1419949-20-4.mol
NVP-TNKS656 Property
  • 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
  • UNSPSC Code 12352200
  • NACRES NA.77
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H400-H410
  • Precautionary statements P264-P270-P273-P301+P312-P330-P391-P501

NVP-TNKS656 Chemical Properties,Usage,Production

  • Description NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM). 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.
  • Uses 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.
  • 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].
  • IC 50 TNKS2: 6 nM (IC50); PARP2: 32 μM (IC50)
  • 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.
NVP-TNKS656 Preparation Products And Raw materials
Raw materials
Preparation Products
NVP-TNKS656 Suppliers
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NVP-TNKS656 Spectrum
1419949-20-4, NVP-TNKS656Related Search:
  • 抑制剂
  • 合成有机化合物配体
  • 细胞生物学试剂
  • 化合物NVP-TNKS656,10 MM DMSO 溶液
  • 化合物 NVP-TNKS656
  • N-(环丙基甲基)-2-(4-(4-甲氧基苯甲酰基)哌啶-1-基)-N - ((4-氧代-4,5,7,8-四氢-3H-吡喃并[4,3-D]嘧啶-2-基)甲基)乙酰胺
  • TNKS2抑制剂(NVP-TNKS656)
  • N-环丙基甲基-2-[4-(4-甲氧基苯甲酰基)哌啶-1-基]-N-[(4-氧代-3,5,7,8-四氢-4H-吡喃并[4,3-D]嘧啶-2-基)甲基]乙酰胺
  • 1419949-20-4
  • NVP-TNKS656, 10 mM in DMSO
  • TNKS656(NVP-TNKS656)
  • 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
  • CS-1333
  • TNKS656; TNKS-656;TNKS 656
  • NVP-TNKS656 - TNKS 656
  • 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
  • TNKS656
  • NVP-TNKS656

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