Size : 2mg
Synonyms: MLN7243
| Description | TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM), blocking ubiquitin binding and disrupting both mono-ubiquitin signaling and overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis. |
| Targets & IC50 | panel of cells derived from hematologic and solid tumors:0.006 μM to 1.31 μM (EC50), myeloma cell:25-100 nM, OCI-AML2 cells、TEX cells、U937 cells、 NB4 cells:15-40 nM, MM.1S cells:25 nM, UBA1:1 nM |
| In vitro | METHODS: Seven myeloma cells were treated with TAK-243 (6.25-500 nM) for 24 h. Cell viability was measured by WST-1 Assay. RESULTS: Most myeloma cells are very sensitive to TAK-243 with IC50 of 25-100 nM, e.g. MM1.S cells with IC50 of 25 nM. [1] METHODS: Human colorectal cancer cells HCT-116 were treated with TAK-243 (0.008-1 µM) for 24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: TAK-243 showed strong selectivity for Sumo and autophagic UBL pathways, and TAK-243 inhibited two E1 enzymes (UBA6 and UAE), which are capable of activating ubiquitin, with equal potency. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, TAK-243 (12.5 mg/kg twice weekly; or 25 mg/kg once weekly) was administered intravenously for two weeks to SCID mice bearing myeloma MM1.S or MOLP-8. S and MOLP-8 models, twice-weekly administration of 12.5 mg/kg produced 60% and 73% tumor growth inhibition at 14 days. 25 mg/kg produced a greater effect. [1] METHODS: To test the antitumor activity in vivo, TAK-243 (20 mg/kg) was injected intravenously twice weekly into SCID mice bearing the human AML tumor OCI-AML2. RESULTS: TAK-243 significantly delayed tumor growth (T/C=0.02) in mice without toxicity. [3] |
| Synonyms | MLN7243 |
| Molecular Weight | 519.52 |
| Formula | C19H20F3N5O5S2 |
| Cas No. | 1450833-55-2 |
| Smiles | NS(=O)(=O)OC[C@H]1C[C@@H](Nc2ccnc3cc(nn23)-c2cccc(SC(F)(F)F)c2)[C@H](O)[C@@H]1O |
| Relative Density. | 1.75 g/cm3 (Predicted) |
| Storage | Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble)  DMSO: 237.5 mg/mL (457.15 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.62 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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