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| 10mg |
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| 25mg |
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Purity: ≥98%
ME0328 (ME-0328) is a novel, potent and selective inhibitor of Poly (ADP-ribose) polymerase (PARP) with potential anticancer activity. It is approximately seven times more selective than PARP1 (IC50 = 6.3 μM) and inhibits PARP3 with an IC50 of 0.89 μM.
| Targets |
ARTD3/PARP3 ( IC50 = 0.89 μM ); ARTD1/PARP1 ( IC50 = 6.3 μM ); ARTD2/PARP2 ( IC50 = 10.8 μM ); ARTD6/TNKS2 ( IC50 = 34.3 μM ); ARTD5/TNKS1 ( IC50 = 47.3 μM ); ARTD10/PARP10 ( IC50 = 71.3 μM )
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| Enzyme Assay |
ARTD proteins tagged with hexahistidine and recombinant histone proteins captured on 96-well Ni2+-chelating plates (5-PRIME) are used to measure protein ADP-ribosylation. NAD+ (2% biotinylated) is added to initiate ADP-ribosylation reactions, and chemiluminescence is used to identify the altered reaction products. Plots of starting rates against NAD+ concentrations and linear curve fitting with GraphPad Prism are used to estimate km values. Dimethyl sulfoxide (DMSO) is used to dissolve each compound to a stock concentration of 50 millimolar. In order to find the IC50 values, experiments are carried out using 1% (v/v) DMSO concentration and compound concentrations ranging from 10 nM to 450 μM. For every transferase, measurements are performed at a concentration of NAD+ less than Km. GraphPad Prism is used to fit curves in order to estimate IC50 values. The values that are reported are the means ± standard error of the curve fits obtained from duplicate or triplicate experiments, with each experiment being determined using three replicates.
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| Cell Assay |
MRC5 and A549 cells are used to test compounds for cytotoxicity using WST-1 assays. Dulbecco's Modified Eagle's Medium, enhanced with 10% fetal calf serum (FCS), penicillin, and streptomycin, is used to cultivate A549 cells. Minimal Essential Medium, which is enhanced with 10% FCS, penicillin, streptomycin, and l-glutamine, is used to cultivate MRC5 cells. Both cell lines are kept at 37°C with 5% CO2 in a humidified incubator.
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| References |
| Molecular Formula |
C19H19N3O2
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| Molecular Weight |
321.37
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| Exact Mass |
321.15
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| Elemental Analysis |
C, 71.01; H, 5.96; N, 13.08; O, 9.96
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| CAS # |
1445251-22-8
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C[C@@H](C1=CC=CC=C1)NC(=O)CCC2=NC3=CC=CC=C3C(=O)N2
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| InChi Key |
QIHBWVVVRYYYRO-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C19H19N3O2/c1-13(14-7-3-2-4-8-14)20-18(23)12-11-17-21-16-10-6-5-9-15(16)19(24)22-17/h2-10,13H,11-12H2,1H3,(H,20,23)(H,21,22,24)/t13-/m0/s1
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| Chemical Name |
3-(4-oxo-3H-quinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide
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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: ≥ 2.5 mg/mL (7.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5%DMSO Corn oil: 1.75mg/ml (5.45mM) (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1117 mL | 15.5584 mL | 31.1168 mL | |
| 5 mM | 0.6223 mL | 3.1117 mL | 6.2234 mL | |
| 10 mM | 0.3112 mL | 1.5558 mL | 3.1117 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.
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