TI-61987
TI-61987 is a TNKS1/2 inhibitor. TI-61987 inhibits TNKS1 and TNKS2 with IC50 values of 7.3 nM and 12 nM, respectively, stabilizes AXIN, and reduces active β-catenin. TI-61987 exhibits weak inhibitory activity against PARP1 and PARP2 enzymatic activity. TI-61987 can be used for research on colorectal cancer.
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- CAS No.: 3043725-09-0
- Formule: C18H14N4O3
- Masse moléculaire:334.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
TNKS1 7.3 nM (IC50) |
TNKS2 12 nM (IC50) |
AXIN |
β-catenin |
PARP1 960 nM (IC50) |
PARP2 140 nM (IC50) |
In Vitro
TI-61987 is a potent TNKS1/2 inhibitor with an IC50 value of 7.3 nM for TNKS1 and 12 nM for TNKS2 in a cell-free colorimetric assay, and shows weaker activity against PARP1 and PARP2[1].
TI-61987 (1 µM) inhibits Wnt/β-catenin TCF/LEF reporter activity in HEK293 cells with an IC50 of 310 nM[1].
TI-61987 (5-20 µM; 10 days) inhibits colony formation in COLO320DM and DLD-1 cells, but not in SW480 cells[1].
TI-61987 (10 µM; 7 days) inhibits COLO320DM 3D spheroid growth[1].
TI-61987 in combination with 5-FU (5-Fluorouracil) (HY-90006), LY294002 (HY-10108), U0126 (HY-12031A), or AZD6244 (Selumetinib) (HY-50706) enhances the growth inhibitory effect on DLD-1, HCT116, and SW480 cells, with cell line-dependent effects[1].
TI-61987 (0.1-10 µM; 24 h) inhibits β-catenin target gene mRNA in COLO320DM cells, induces AXIN2, and decreases active β-catenin protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:COLO320DM, DLD-1, SW480
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Concentration:5-20 µM TI-61987
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Incubation Time:10 days
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Result:Inhibited the growth of COLO320DM and DLD-1 cells but did not substantially affect SW480 cells.
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Cell Line:COLO320DM cells
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Concentration:0.1 μM; 1 μM; 10 μM
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Incubation Time:24 h
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Result:Reduced the level of active β-catenin protein.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu/nu (BALB/c nude; 6-week-old)[1]
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Dosage:20 mg/kg; 50 mg/kg
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Administration:intraperitoneally; three times per week (also every other day); 14 days
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Result:Reduced tumor growth by 43.9% at 20 mg/kg and 53% at 50 mg/kg compared with the vehicle group.
No pronounced differences in body weight were observed between vehicle- and TI-61987-treated mice.
Tumors from TI-61987-treated mice exhibited markedly increased AXIN2 expression and reduced active β-catenin levels by immunohistochemistry compared with controls.
No damage to crypts or villi was observed in the small intestine of TI-61987-treated mice, and intestines appeared comparable with those of the control group.
Chemical Information
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CAS No. 3043725-09-0
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Masse moléculaire 334.33
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Formule C18H14N4O3
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SMILES
O=C(NC1=C2C=CNC2=CC=C1)CN3NC(C4=CC=CC=C4C3=O)=O
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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)
TI-61987 Related Classifications
HY-189723 Related Classifications
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