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L-779450

Catalog No. T1953 CAS 303727-31-3

Synonyms: 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.

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L-779450, CAS 303727-31-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 42.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 109.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 597.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 98%

Biological Description

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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.

Synonyms	L 779450
Molecular Weight	347.8
Formula	C20H14ClN3O
CAS No.	303727-31-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (172.51 mM)

References and Literature

1. Shelton JG, et al. Leukemia. 2003 Sep;17(9):1765-82.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Ovarian Cancer Compound Library MAPK Inhibitor Library Anti-Pancreatic Cancer Compound Library HIF-1 Signaling Pathway Compound Library Bioactive Compound Library NO PAINS Compound Library Reprogramming Compound Library Anti-Liver Cancer Compound Library

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Keywords

L-779450 303727-31-3 Autophagy MAPK Raf Raf kinases L 779450 Inhibitor L779450 inhibit inhibitor

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