Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
eIF4A3-IN-2 (Compound 2) binds to the allosteric region of eIF4A3 and, in vitro, inhibits the activities of ATPase, helicase, and cellular nonsense-mediated RNA decay (NMD) [1].
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Cell Assay |
Apoptosis analysis [1]
Cell Types: HEK293T cells (transfected with NMD reporter gene) Luciferase assay Tested Concentrations: 0.3, 1, 3 or 10 μM Incubation Duration: 3 or 6 hrs (hours) Experimental Results: eIF4A3-IN-2 induces apoptosis The luciferase activity increased approximately 3.2 times, indicating that NMD was inhibited by compound 2[1]. |
References |
Molecular Formula |
C25H19BR2CLN4O2
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Molecular Weight |
602.704962968826
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Exact Mass |
601.954
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CAS # |
2095677-20-4
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Related CAS # |
(R)-eIF4A3-IN-2;2095484-82-3
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PubChem CID |
131953885
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Appearance |
White to light yellow solid powder
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LogP |
5
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
3
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Rotatable Bond Count |
3
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Heavy Atom Count |
34
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Complexity |
744
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Defined Atom Stereocenter Count |
1
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SMILES |
BrC1C=CC2=C(C=NN2C=1)C(N1CCN(C(C2C=CC(=CC=2)Br)=O)[C@@H](C2C=CC(=CC=2)Cl)C1)=O
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InChi Key |
WKKAVTNXNVPCCN-HSZRJFAPSA-N
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InChi Code |
InChI=1S/C25H19Br2ClN4O2/c26-18-5-1-17(2-6-18)24(33)31-12-11-30(15-23(31)16-3-8-20(28)9-4-16)25(34)21-13-29-32-14-19(27)7-10-22(21)32/h1-10,13-14,23H,11-12,15H2/t23-/m1/s1
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Chemical Name |
(4-bromophenyl)-[(2S)-4-(6-bromopyrazolo[1,5-a]pyridine-3-carbonyl)-2-(4-chlorophenyl)piperazin-1-yl]methanone
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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 |
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) |
DMSO : ~100 mg/mL (~165.92 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.15 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (2.77 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 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (2.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6592 mL | 8.2959 mL | 16.5917 mL | |
5 mM | 0.3318 mL | 1.6592 mL | 3.3183 mL | |
10 mM | 0.1659 mL | 0.8296 mL | 1.6592 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.