Details
Stereochemistry | ACHIRAL |
Molecular Formula | C27H34N4O5 |
Molecular Weight | 494.5827 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(C=C1)C(=O)C2CCN(CC(=O)N(CC3CC3)CC4=NC(=O)C5=C(CCOC5)N4)CC2
InChI
InChIKey=DYGBNAYFDZEYBA-UHFFFAOYSA-N
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)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23844574
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23844574
NVP-TNKS656 was identified as an orally active selective tankyrase 2 (TNKS2) inhibitor, which is also antagonist of Wnt pathway activity. On animal models for Colorectal Cancer was shown, that NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23844574
Curator's Comment: # Novartis Institutes for Biomedical Research, Inc
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL6154 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23844574 |
6.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
MMTV-Wnt1 tumor bearing athymic nude mice: NVP-TNKS656: 350 mg/kg, p.o.
mice bearing SW480 xenografts: twice daily with vehicle, NVP-TNKS656 (100 mg/kg, subcutaneous injection) or AZD6244 (45 mg/kg, oral) for the duration of the study.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26224873
Combination with NVP-TNKS656 promoted apoptosis in PI3K or AKT inhibitor-resistant cells with high nuclear β-catenin content. High FOXO3A activity conferred sensitivity to NVP-TNKS656 treatment. Patient-derived cells were treated with NVP-TNKS656 100 nmol/L for 7 days and eGFP accumulation was measured by flow cytometry.
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136237316
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SUBSTANCE RECORD