Product Name :
NVP-TNKS656, Wnt / Tankyrase Inhibitor
Description:
NVP-TNKS656 is a highly potent, selective and oral bioavailable tankyrase inhibitor with IC50 of 6 nM for TNKS2. It has 300-fold selectivity against PARP1 and PARP2. In MMTV-Wnt1 tumor models, NVP-TNKS656 was dosed to mice orally to stabilize Axin1 protein and reduce the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.
CAS:
1419949-20-4
Molecular Weight:
494.58
Formula:
C27H34N4O5
Chemical Name:
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
Smiles :
COC1=CC=C(C=C1)C(=O)C1CCN(CC(=O)N(CC2NC(=O)C3COCCC=3N=2)CC2CC2)CC1
InChiKey:
DYGBNAYFDZEYBA-UHFFFAOYSA-N
InChi :
InChI=1S/C27H34N4O5/c1-35-21-6-4-19(5-7-21)26(33)20-8-11-30(12-9-20)16-25(32)31(14-18-2-3-18)15-24-28-23-10-13-36-17-22(23)27(34)29-24/h4-7,18,20H,2-3,8-17H2,1H3,(H,28,29,34)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Vipivotide tetraxetan} web|{Vipivotide tetraxetan} Drug-Linker Conjugates for ADC|{Vipivotide tetraxetan} Technical Information|{Vipivotide tetraxetan} Formula|{Vipivotide tetraxetan} manufacturer|{Vipivotide tetraxetan} Epigenetic Reader Domain}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Cedazuridine} MedChemExpress|{Cedazuridine} Biological Activity|{Cedazuridine} In Vitro|{Cedazuridine} custom synthesis|{Cedazuridine} Epigenetics}
Additional information:
NVP-TNKS656 is a highly potent, selective and oral bioavailable tankyrase inhibitor with IC50 of 6 nM for TNKS2.PMID:24268253 It has 300-fold selectivity against PARP1 and PARP2. In MMTV-Wnt1 tumor models, NVP-TNKS656 was dosed to mice orally to stabilize Axin1 protein and reduce the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.|Product information|CAS Number: 1419949-20-4|Molecular Weight: 494.58|Formula: C27H34N4O5|Synonym:|TNKS656|Chemical Name: 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|Smiles: COC1=CC=C(C=C1)C(=O)C1CCN(CC(=O)N(CC2NC(=O)C3COCCC=3N=2)CC2CC2)CC1|InChiKey: DYGBNAYFDZEYBA-UHFFFAOYSA-N|InChi: InChI=1S/C27H34N4O5/c1-35-21-6-4-19(5-7-21)26(33)20-8-11-30(12-9-20)16-25(32)31(14-18-2-3-18)15-24-28-23-10-13-36-17-22(23)27(34)29-24/h4-7,18,20H,2-3,8-17H2,1H3,(H,28,29,34)|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 100 mM; EtOH up to 100 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|NVP-TNKS656 was used at 10 µM in vitro and cellular assays.|In Vivo:|In MMTV-Wnt1 tumor bearing athymic nude mice, NVP-TNKS656 was dosed to mice orally at 100-350 mg/Kg once per day to stabilize Axin1 protein and reduce the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.|References:|Shultz MD, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. (2013) J Med Chem. 56(16):6495-511.Arqués O, et al. Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer. (2016) Clin Cancer Res. 22(3):644-56.Products are for research use only. Not for human use.|Documents||
