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L-779450

L-779450
L-779450, an effective, ATP-competitive Raf kinase inhibitor (IC50: 10 nM) , displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.
Catalog No. T1953Cas No. 303727-31-3
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Purity:98%
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L-779450

Catalog No. T1953Cas No. 303727-31-3
L-779450, an effective, ATP-competitive Raf kinase inhibitor (IC50: 10 nM) , displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.
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Pack SizePriceAvailabilityQuantity
2 mg$42In Stock
5 mg$67In Stock
10 mg$109In Stock
25 mg$198In Stock
50 mg$372In Stock
100 mg$597In Stock
1 mL x 10 mM (in DMSO)$75In Stock
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Product Introduction

Bioactivity
Description
L-779450, an effective, ATP-competitive Raf kinase inhibitor (IC50: 10 nM) , displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.
Targets&IC50
Raf kinase:10 nM
Kinase Assay
Akt kinases assay: Akt kinases are assayed by a GSK-derived biotinylated peptide substrate. The extent of peptide phosphorylation is determined by Homogeneous Time Resolved Fluorescence (HTRF) using a lanthanide chelate (Lance)-coupled monoclonal antibody specific for the phosphopeptide in combination with a streptavidin-linked allophycocyanin (SA-APC) fluorophore which will bind to the biotin moiety on the peptide. When the Lance and APC are in proximity, a non-radiative energy transfer takes place from the Lance to the APC, followed by emission of light from APC at 655 nm. Working Solution: 100X protease inhibitor cocktail (PIC): 1 mg/mL benzamidine, 0.5 mg/mL pepstatin, 0.5 mg/mL leupeptin, 0.5 mg/mL aprotinin; 10X assay buffer: 500 mM HEPES, pH7.5, 1% PEG, 16.6 mM EDTA, 1 mM EGTA, 1% BSA, 20 mM 9-glycerol phosphate; Quench buffer 50 mM HEPES pH 7.3, 16.6 mM EDTA, 0.1% BSA, 0.1% Triton X-100, 0.17 nM labeled monoclonal antibody, 0.0067 mg/mL SA-APC; ATP/MgCl2 working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, active Akt; Peptide working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, 2 TM GSK biotinylated peptide. The reaction is assembled by adding 16 μL of ATP/MgCl2 working solution to the appropriate wells. MK-2206 or vehicle (1.0 μL) is added followed by 10 μL of peptide working solution. The reaction is started by adding 13 μL of the enzyme working solution and mixing. The reaction is allowed to proceed for 50 min and then stopped by the addition of 60 μL HTRF quench buffer. The stopped reactions are incubated at room temperature for at least 30 min and then read in the instrument.
AliasL 779450
Chemical Properties
Molecular Weight347.8
FormulaC20H14ClN3O
Cas No.303727-31-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (172.51 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.8752 mL14.3761 mL28.7522 mL143.7608 mL
5 mM0.5750 mL2.8752 mL5.7504 mL28.7522 mL
10 mM0.2875 mL1.4376 mL2.8752 mL14.3761 mL
20 mM0.1438 mL0.7188 mL1.4376 mL7.1880 mL
50 mM0.0575 mL0.2875 mL0.5750 mL2.8752 mL
100 mM0.0288 mL0.1438 mL0.2875 mL1.4376 mL

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