bs-60328C
[Life Science]
NVP-TNKS656, Wnt / Tankyrase Inhibitor
DATASHEET
Formulation Powder
Storage: Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 494.58
Formula: C27 H34 N4 O5
CAS Number: 1419949-20-4
InChi Key: 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)
Smiles: COC1=CC=C(C=C1)C(=O)C1CCN(CC(=O)N(CC2NC(=O)C3COCCC=3N=2)CC2CC2)CC1
Purity: 98.0
Solubility: DMSO up to 100 mM; EtOH up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Formula: C27 H34 N4 O5
CAS Number: 1419949-20-4
InChi Key: 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)
Smiles: COC1=CC=C(C=C1)C(=O)C1CCN(CC(=O)N(CC2NC(=O)C3COCCC=3N=2)CC2CC2)CC1
Purity: 98.0
Solubility: DMSO up to 100 mM; EtOH up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
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.
Size: 10mg solid, 2 mg solid10mg solid, 2 mg solid
Applications: Life Science()
For research use only. Not intended for diagnostic or therapeutic use.