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R-406

Cat. No. M1767
R-406 Structure
Size Price Availability Quantity
10mg USD 185 In stock
50mg USD 625 In stock
100mg USD 1000 In stock
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Quality Control
Biological Activity

R406 is an orally bioavailable and selective inhibitor of spleen tyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30 nM. R406 is an active component of its prodrug R788 or R935788 (Fostamatinib).

Protocol
Cell Experiment
Cell lines CLL cells
Preparation method To evaluate the effect of BCR stimulation on CLL cell viability, CLL cells (107/mL) were incubated in complete RPMI medium (control) or in complete medium supplemented with 10 μg/mL anti-IgM (polyclonal goat F(ab′)2 fragments to human IgM [MP Biomedicals] at 37°C in 5% CO2). After 24 and 48 hours, CLL cell viability was measured by analysis of mitochondrial transmembrane potential by 3,3 dihexyloxocarbocyanine iodine (DiOC6; Invitrogen-Molecular Probes) and cell membrane permeability to propidium iodide (PI; Molecular Probes), as described.13 Briefly, 200 μL cell suspension was collected at the indicated time points and transferred to fluorescence-activated cell sorter tubes containing 200 μL of 60 nM DiOC6 and 2 μg/mL PI in RPMI with 0.5% bovine serum albumin. Cells were then incubated at 37°C for 15 minutes and analyzed within 30 minutes by flow cytometry on a FACSCalibur (BD Biosciences).
Concentrations 5 μM
Incubation time 24 and 48 h
Animal Experiment
Animal models K/BxN Model in C57BL/6 mice
Formulation 35% TPGS, 60% PEG 400, and 5% propylene glycol
Dosages b.i.d for 13 days
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 470.45
Formula C22H23FN6O5
CAS Number 841290-80-0
Purity >99%
Solubility DMSO ≥29 mg/mL
Storage at -20°C
References

B-cell antigen receptor signaling enhances chronic lymphocytic leukemia cell migration and survival: specific targeting with a novel spleen tyrosine kinase inhibitor, R406.
Quiroga MP, et al. Blood. 2009 Jul 30;114(5):1029-37. PMID: 19491390.

Fostamatinib, a Syk inhibitor prodrug for the treatment of inflammatory diseases.
Bajpai M. IDrugs. 2009 Mar;12(3):174-85. PMID: 19333898.

R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.
Braselmann S, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. PMID: 16946104.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: R-406 supplier, Syk, inhibitors

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