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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
G007-LK is a novel, potent and specific tankyrase (TNKS) 1/2 inhibitor with potential anticancer activity. Its respective IC50s for inhibiting TNKS 1/2 are 46 nM and 25 nM. ADP ribosylation of TNKS1 and TNKS2 was decreased by G007-LK. In vivo antitumor efficacy is also high, and it exhibits strong antiproliferative activity against a variety of cancer cells. G007-LK has an IC50 value of 0.05 μM and inhibits ST-Luc in HEK 293 cells that have been induced with Wnt3a. Using the GFP-TNKS1-transfected SW480 colorectal cancer cell line, G007-LK generates phosphorylated beta-catenin, beta-TrCP, and ubiquitin-containing highly dynamic and mobile degradasomes. G007-LK lowers nuclear and cytosolic β-catenin protein levels in the APC-mutant cell lines.
Targets |
TNKS2 ( IC50 = 25 nM ); TNKS1 ( IC50 = 46 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
TNKS1 and TNKS2 in vitro biochemical assays: G007-LK inhibitory activity is examined twice against TNKS1, TNSK2 Chemiluminescent Assay Kits at different dosages (duplicates), and the luminescence is gauged using a GloMax Luminometer.
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Cell Assay |
In order to conduct assays on cell proliferation or apoptosis, SNU-449 and HLE cells are cultured in RPMI Medium supplemented with 10% fetal bovine serum (FBS), penicillin/streptomycin, and 5% CO2 at 37°C. Treatment options for HCC cells include 0.1% DMSO, 2.5 μM, 5 μM, 10 μM, 20 μM XAV-939 or G007-LK, either by itself or in combination with the AKT inhibitor MK-2206 (5 μM) or the MEK inhibitor U0126 (25 μM). The Cell Death Detection Elisa Plus Kit is used to measure apoptosis, and the BrdU Cell Proliferation Assay Kit is used to analyze cell proliferation[3].
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Animal Protocol |
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References |
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Molecular Formula |
C25H16CLN7O3S
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Molecular Weight |
529.96
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Exact Mass |
529.072
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Elemental Analysis |
C, 56.66; H, 3.04; Cl, 6.69; N, 18.50; O, 9.06; S, 6.05
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CAS # |
1380672-07-0
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Related CAS # |
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PubChem CID |
67960134
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Appearance |
Off-white to yellow solid powder
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LogP |
5.559
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
9
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Rotatable Bond Count |
6
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Heavy Atom Count |
37
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Complexity |
961
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Defined Atom Stereocenter Count |
0
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SMILES |
ClC1=C([H])C([H])=C([H])C([H])=C1N1C(/C(/[H])=C(\[H])/C2=NN=C(C3C([H])=C([H])C(C#N)=C([H])C=3[H])O2)=NN=C1C1C([H])=C([H])C(=C([H])N=1)S(C([H])([H])[H])(=O)=O
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InChi Key |
HIWVLHPKZNBSBE-OUKQBFOZSA-N
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InChi Code |
InChI=1S/C25H16ClN7O3S/c1-37(34,35)18-10-11-20(28-15-18)24-31-29-22(33(24)21-5-3-2-4-19(21)26)12-13-23-30-32-25(36-23)17-8-6-16(14-27)7-9-17/h2-13,15H,1H3/b13-12+
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Chemical Name |
4-[5-[(E)-2-[4-(2-chlorophenyl)-5-(5-methylsulfonylpyridin-2-yl)-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.92 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.