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G007-LK PARP inhibitor

Name: G007-LK
Brand: Selleck Chemicals
SKU: S7239
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S7239

G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.

Chemical Structure

Molecular Weight: 529.96

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.83%

99.83

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HEK293	Function assay		24 hrs		Inhibition of TNKS1/2 in HEK293 cells assessed as inhibition of Wnt/beta-casein pathway after 24 hrs by luciferase reporter gene assay, IC50 = 0.05 μM.	23473363
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	529.96	Formula	C₂₅H₁₆ClN₇O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1380672-07-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CS(=O)(=O)C1=CN=C(C=C1)C2=NN=C(N2C3=CC=CC=C3Cl)C=CC4=NN=C(O4)C5=CC=C(C=C5)C#N

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (130.19 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	TNKS2 ^[1] (Cell-free assay) 25 nM TNKS1 ^[1] (Cell-free assay) 46 nM
In vitro	G007-LK reduces Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization. This compound 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. It (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%. This chemical suppresses colony formation in CRC lines COLO-320DM and SW403. It suppresses organoids growth with IC50 of 80 nM. ^[2]
Kinase Assay	TNKS1 and TNKS2 in vitro biochemical assays
Kinase Assay	G007-LK inhibitory activity at various doses (duplicates) is tested twice against TNKS1, TNSK2 Chemiluminescent Assay Kits, and the luminescence is measured on a GloMax Luminometer.
In vivo	G007-LK exhibits antitumor efficacy in xenograft and genetically engineered CRC models. In the COLO-320DM model, this compound 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. This compound treatment increases expression of KRT20 and TM4SF4 in COLO-320DM tumors. It (20 mg/kg twice daily) achieves 61% tumor growth inhibition. This chemical reduces Wnt/β-catenin signaling and cell proliferation in normal intestine. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/23473363/ [2] https://pubmed.ncbi.nlm.nih.gov/23539443/

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