| Size | Price | Stock | Qty |
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| 1mg |
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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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| Other Sizes |
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| Targets |
mTOR ( IC50 = 0.6 nM ); ATR ( IC50 = 14 nM ); ATM ( IC50 = 545 nM ); DNA-PK ( IC50 = 36 nM ); PI3Kα ( IC50 = 170 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Compounds (e.g., ETP-46464) and master suppressors are introduced straight into the cell medium (100 μL in each well) using a multi-well pipette, with an ultimate concentration of 10 μM. By meticulously vortexing plates at 500 rpm, media content is homogenized. Before adding 4-hydroxy-tamoxifen (4-OHT), compounds (like ETP-46464) are incubated for 15 minutes at 37ºC. All wells are then treated with 4-OHT and incubated for 60 minutes at 37ºC to trigger ATR activity. Cells are then prepared for IF after being fixed with paraformaldehyde. Each compound (such as ETP-46464) undergoes at least three separate experiments for analysis[1].
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| Cell Assay |
The cells are plated in 96-well plates at 5000 cells per well for KLE, HEC1B, and HELA, and 10,000 cells per well for OVCAR3, A2780, A2780-CP20, and SIHA. The cells are trypsinized with 0.25% Trypsin-EDTA, and they are counted with 0.4% Trypan Blue using an automated cell counter. Following 24-48 hours after seeding, the media is removed and replaced with new media containing either 0.78, 1.56, 3.13, 6.25, 12.5, 25, 50, or 100 µM of Cisplatin or 0.56, 3.13, 6.25, 12.5, 25, 50, or 100 µM of Carboplatin in 0.15% DMSO, 5 µM ETP-46464, 10 µM KU55933, or a combination of 5 µM ETP-46464 and 10 µM KU55933 and incubated for 72 hours. The final ETP-46464 and KU55933 concentrations used are determined by previous data showing inhibition of ATR and ATM signaling, respectively. In a subset of cell lines, single-agent dose response analyses of ETP-46464 and KU55933 showed a broad LD50 range (10.0±8.7 and 38.3±7.6 µM, respectively). In a similar manner, new media containing ciprofloxacin (0, 0.78, 1.56, 3.13, 6.25, 12.5, 25 or 50 µM) in 0.08% DMSO and 5 µM VE-821 are applied to the cells. The MTS CellTiter 96 Aqueous One Solution Cell Proliferation Assay is used to determine the viability of cells. A microplate spectrophotometer is used to measure absorbance at 490 nm following a 2-hour incubation period at 37°C. For every cell line, three biological replicates are carried out, and each experiment's inhibitor(s) and/or ciplatin concentration is measured in triplicate[2].
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| Animal Protocol |
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| References |
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| Molecular Formula |
C30H22N4O2
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| Molecular Weight |
470.52
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| Exact Mass |
470.17
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| Elemental Analysis |
C, 76.58; H, 4.71; N, 11.91; O, 6.80
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| CAS # |
1345675-02-6
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| Related CAS # |
1345675-02-6
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3COC2=O)C5=CC6=CC=CC=C6N=C5
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| InChi Key |
DPLMXAYKJZOTKO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H22N4O2/c1-30(2,18-31)23-8-10-24(11-9-23)34-28-22(17-36-29(34)35)16-33-27-12-7-19(14-25(27)28)21-13-20-5-3-4-6-26(20)32-15-21/h3-16H,17H2,1-2H3
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| Chemical Name |
2-methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile
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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: ≥ 0.5 mg/mL (1.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 5.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1253 mL | 10.6265 mL | 21.2531 mL | |
| 5 mM | 0.4251 mL | 2.1253 mL | 4.2506 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1253 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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