A TNKS1/2 inhibitor (IC50s = 46 and 25 nM

G007-LK – 10 mg

Brand:
Cayman
CAS:
1380672-07-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

G007-LK is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 46 and 25 nM, respectively).{40726} It is selective for TNKS1 and TNKS2 over a panel of 90 kinases, 16 phosphatases, and 73 G protein-coupled receptors (GPCRs) when used at a concentration of 10 µM. G007-LK inhibits colony formation of COLO 320 DM and SW403 colorectal cancer cell lines when used at a concentration of 200 µM, as well as human hepatocellular carcinoma (HCC) cells in a dose-dependent manner.{40727,40728} It increases expression of intestinal differentiation markers in COLO 320 DM and HCT15 cells when used at a concentration of 100 nM. G007-LK inhibits Wnt3A-induced signaling in human HEK293 and mouse 10T1/2 cells.{40727} G007-LK (20 mg/kg, i.p., twice daily) also inhibits tumor growth in COLO 320 DM and SW403 mouse xenograft models, however, it leads to intestinal toxicity when administered at a dose of 30 mg/kg twice daily, leading to moribundity and death.  

 

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SKU: 22934 - 10 mg Category:

Description

A TNKS1/2 inhibitor (IC50s = 46 and 25 nM, respectively); selective for TNKS1 and TNKS2 over a panel of 90 kinases, 16 phosphatases, and 73 GPCRs; inhibits colony formation of COLO 320 DM and SW403 cells (200 µM); inhibits colony formation of HCC cells in a dose-dependent manner; increases differentiation marker expression in COLO 320 DM and HCT15 cells (100 nM); inhibits Wnt signaling in HEK293 and 10T1/2 cells in a dose-dependent manner; inhibits tumor growth in COLO 320 DM and SW403 mouse xenograft models (20 mg/kg, i.p., twice daily) but leads to moribundity and death at a dose of 30 mg/kg twice daily

Formal name: 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-benzonitrile

Synonyms:  Tankyrase 1/2 Inhibitor VI

Molecular weight: 530

CAS: 1380672-07-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cancer|DNA Damage and Repair|PARP||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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