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PLX647

Catalog No. T1925   CAS 873786-09-5

PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).

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PLX647 Chemical Structure
PLX647, CAS 873786-09-5
Pack Size Availability Price/USD Quantity
2 mg 5 days $ 38.00
5 mg 5 days $ 59.00
1 mL * 10 mM (in DMSO) 5 days $ 58.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).
Targets&IC50 Kit:16 nM, FMS:28nM
Kinase Assay HTS screen: To start an assay, 0.5 μL of 5 mg/mL test compound (about 50 μM final reaction concentration) or DMSO control is aliquoted into each well. Both enzyme and substrate are prepared in UCH reaction buffer (50 mM Tris-HCl [pH 7.6], 0.5 mM EDTA, 5 mM DTT, and 0.5 mg/mL ovalbumin). 25 μL of 0.6 nM UCH-L1 is then added to each well except substrate control wells, followed by plate shaking for 45–60 s on an automatic shaker. The enzyme/compound mixture is incubated at room temperature for 30 min before 25 μL of 200 nM Ub-AMC is added to initiate the enzyme reaction. The reaction mixture (300 pM UCH-L1, 100 nM Ubiquitin-AMC with 2.5 μg test compound) is incubated at room temperature for 30 additional minutes prior to quenching the reaction by the addition of 10 μL 500 mM acetic acid per well. The fluorescence emission intensity is measured on a LJL Analyst using a coumarin filter set (ex = 365 nm, em = 450 nm) and is subtracted by the intrinsic compound fluorescence to reveal the enzyme activity. A DMSO control (0.5 μL of DMSO, 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), enzyme control (25 μL of UCH-L1, 25 μL of buffer, 10 μL of acetic acid), substrate control (25 μL of buffer, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), and inhibitor control (0.5 μL of ubiquitin aldehyde [100 nM stock], 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid) are also performed in each assay plate to ensure quality and reproducibility. Potential UCH-L1 inhibitors are selected if the compounds demonstrated greater than 60% inhibition compared to the controls. The UCH-L1 enzymatic reactions are manually repeated twice using the same protocol to confirm the results for the hit compounds from the primary robot-assisted screen.
Molecular Weight 382.38
Formula C21H17F3N4
CAS No. 873786-09-5

Storage

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

Solubility Information

DMSO: 31 mg/mL

TargetMolReferences and Literature

1. Zhang C, et al. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94.

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Keywords

PLX647 873786-09-5 Tyrosine Kinase/Adaptors c-Kit c-Fms Inhibitor cells osteoclast SCFR BCR-FMS CD117 bone PLX-647 differentiation colony stimulating factor 1 receptor BCR-KIT PLX 647 CSF1R inhibit CSF-1 receptor proliferation CSF-1R inhibitor

 

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