Size | Price | Stock | Qty |
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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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Other Sizes |
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Purity: ≥98%
AGI-6780 (AGI6780; AGI 6780) is a potent and selective inhibitor of tumor-associated mutant IDH2 (isocitrate dehydrogenases 2) R140Q with potential anti-inflammatory activity. It inhibits IDH2 R140Q with an IC50 of 23 nM. It shows less potency against IDH2(WT) with an IC50 of 190±8.1 nM.
ln Vitro |
Human glioblastoma U87 and TF-1 cells expressing IDH2R140Q are tested for AGI-6780, with IC50 values of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectively, after 48 hours of incubation. When AGI-6780 is administered to TF-1R140Q cells at concentrations that bring down 2HG to nearly normal physiological levels, both the expression of the HBG and KLF1 genes as well as the differentiation-associated color change are restored. In TF-1 cells, AGI-6780 can undo the differentiation block caused by IDH2R140Q. Before undergoing EPO-induced differentiation, the TF1R140Q cells' intracellular concentration of (R)-2-hydroxyglutarate was significantly reduced by pretreatment with AGI-6780 (0.2 μM and 1 μM)[1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Wang F, et al. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science. 2013 May 3;340(6132):622-6
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Molecular Formula |
C21H18F3N3O3S2
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Molecular Weight |
481.51
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CAS # |
1432660-47-3
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Related CAS # |
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=S(C1=CC=C(C2=CSC=C2)C(NC(NC3=CC=CC(C(F)(F)F)=C3)=O)=C1)(NC4CC4)=O
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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 (5.19 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: ≥ 2.5 mg/mL (5.19 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 25.0 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 | 2.0768 mL | 10.3840 mL | 20.7680 mL | |
5 mM | 0.4154 mL | 2.0768 mL | 4.1536 mL | |
10 mM | 0.2077 mL | 1.0384 mL | 2.0768 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.