TNKS-IN-4
TNKS-IN-4 (compound 49) is an orally active tankyrase (TNKS) inhibitor with IC50 values of 0.1 nM and 7.6nM for TNKS1 and TNKS2, respectively. TNKS-IN-4 can be used for study of APC-mutant colorectal cancer.
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- CAS No.: 1507362-06-2
- Formule: C24H24N4O3S
- Masse moléculaire:448.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
TNKS1 0.1 nM (IC50) |
TNKS2 7.6 nM (IC50) |
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | IC50 |
0.3 nM
Compound: 49
|
Inhibition of TNKS in human DLD1 cells expressing APC mutant assessed as inhibition of super-Topflash reporter gene transcription after 40 to 48 hrs by dual-glo luciferase reporter gene assay
Inhibition of TNKS in human DLD1 cells expressing APC mutant assessed as inhibition of super-Topflash reporter gene transcription after 40 to 48 hrs by dual-glo luciferase reporter gene assay
|
[PMID: 24294969] |
| SW480 | EC50 |
4 nM
Compound: 49
|
Inhibition of TNKS in human SW480 cells assessed as accumulation of axin-2 into cytoplasmic foci after 24 hrs by Hoechst dye-based assay
Inhibition of TNKS in human SW480 cells assessed as accumulation of axin-2 into cytoplasmic foci after 24 hrs by Hoechst dye-based assay
|
[PMID: 24294969] |
| SW480 | IC50 |
1.9 nM
Compound: 49
|
Inhibition of TNKS in human SW480 cells assessed as degradation of total pool of beta-catenin after 40 to 48 hrs
Inhibition of TNKS in human SW480 cells assessed as degradation of total pool of beta-catenin after 40 to 48 hrs
|
[PMID: 24294969] |
Chemical Information
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CAS No. 1507362-06-2
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Masse moléculaire 448.54
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Formule C24H24N4O3S
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SMILES
O=C1C2=CC=CC=C2NC(SCCC(N[C@@H]3CC[C@@H](OC4=CC=C(C#N)C=C4)CC3)=O)=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)