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TAK-580

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Catalog No. T6895Cas No. 1096708-71-2
Alias Tovorafenib, MLN2480, BIIB-024

TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.

TAK-580

TAK-580

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Purity: 99.77%
Catalog No. T6895Alias Tovorafenib, MLN2480, BIIB-024Cas No. 1096708-71-2
TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$48In StockIn Stock
5 mg$105In StockIn Stock
10 mg$169In StockIn Stock
25 mg$313In StockIn Stock
50 mg$463In StockIn Stock
100 mg$683-In Stock
1 mL x 10 mM (in DMSO)$118In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.77%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.
In vitro
TAK-580 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preClinicalal cancer models at concentrations that are tolerated in vivo. It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts. In vitro analysis of this drug combination of TAK-580 and TAK-733(an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity. In addition, western blot analysis demonstrates the effect of TAK-580 in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition.MLN-2480 only modestly inhibits PRAK.
In vivo
In vivo, TAK-580 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models.MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produces negligible effects.
Animal Research
[4]Animal Models: C57BL/6J miceFormulation: 100% PEG400Dosages: 12.5 mg/kgAdministration: oral gavage
SynonymsTovorafenib, MLN2480, BIIB-024
Chemical Properties
Molecular Weight506.29
FormulaC17H12Cl2F3N7O2S
Cas No.1096708-71-2
SmilesCC(NC(=O)c1ncnc(N)c1Cl)c1ncc(s1)C(=O)Nc1cc(c(Cl)cn1)C(F)(F)F
Relative Density.1.64
Storage & Solubility Information
StoragePowder: -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: 93 mg/mL (183.69 mM), Sonication is recommended.
Ethanol: 93 mg/mL (183.69 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (1.98 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/Ethanol
1mg5mg10mg50mg
1 mM1.9752 mL9.8758 mL19.7515 mL98.7576 mL
5 mM0.3950 mL1.9752 mL3.9503 mL19.7515 mL
10 mM0.1975 mL0.9876 mL1.9752 mL9.8758 mL
20 mM0.0988 mL0.4938 mL0.9876 mL4.9379 mL
50 mM0.0395 mL0.1975 mL0.3950 mL1.9752 mL
100 mM0.0198 mL0.0988 mL0.1975 mL0.9876 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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