[CAS NO. 1380672-07-0] G007-LK
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PRODUCTS SPECIFICATIONS [1380672-07-0]
Store
Catalog
SLK-S7239
Brand
Selleck
CAS
1380672-07-0
DESCRIPTION [1380672-07-0]
Overview
| MDL | MFCD28167833 |
|---|---|
| Molecular Weight | 529.96 |
| Molecular Formula | C25H16ClN7O3S |
| SMILES | ClC1=C(N2C(/C=C/C3=NN=C(O3)C4=CC=C(C=C4)C#N)=NN=C2C5=CC=C(C=N5)S(C)(=O)=O)C=CC=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8869 mL | 9.4347 mL | 18.8693 mL |
| 5 mM | 0.3774 mL | 1.8869 mL | 3.7739 mL |
| 10 mM | 0.1887 mL | 0.9435 mL | 1.8869 mL |
| 50 mM | 0.0377 mL | 0.1887 mL | 0.3774 mL |
Description
G007-LK is a potent and selective inhibitor with of 46 nM and 25 nM for TNKS1/2, respectively.
In vitro
G007-LK reduces Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization. G007-LK completely blocks ligand-driven Wnt/β-catenin signaling in cell culture and display approximately 50% inhibition of APC mutation–driven signaling in most CRC cell lines. G007-LK (0.2 μM) reduces the number of COLO-320DM cells in mitosis from 24% to 12% and decreases HCT-15 cells in S-phase from 28% to 18%. G007-LK suppresses colony formation in CRC lines COLO-320DM and SW403. G007-LK suppresses organoids growth with IC50 of 80 nM.
In vivo
G007-LK exhibits antitumor efficacy in xenograft and genetically engineered CRC models. In the COLO-320DM model, G007-LK reduces tankyrases 1 and tankyrases 2 protein levels, stabilizes AXIN1 and AXIN2, and decreases β-catenin level. Wnt/β-catenin signaling is clearly inhibited in a dose-dependent manner in the efficacy study tumors as indicated by reduced expression of β-catenin–activated genes NKD1, APCDD1, and TNFRSF19 (TROY), as well as increased expression of β-catenin–repressed gene CLIC3. G007-LK treatment increases expression of KRT20 and TM4SF4 in COLO-320DM tumors. G007-LK (20 mg/kg twice daily) achieves 61% tumor growth inhibition. G007-LK reduces Wnt/β-catenin signaling and cell proliferation in normal intestine.
References
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