R406 (free base)

Syk inhibitor CAS# 841290-80-0

R406 (free base)

Catalog No. BCC2553----Order now to get a substantial discount!

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R406 (free base): 5mg $104 In Stock
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Chemical structure

R406 (free base)

3D structure

Chemical Properties of R406 (free base)

Cas No. 841290-80-0 SDF Download SDF
PubChem ID 11213558 Appearance Powder
Formula C22H23FN6O5 M.Wt 470.4
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 10 mg/mL (21.26 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
SMILES CC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C
Standard InChIKey NHHQJBCNYHBUSI-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H23FN6O5/c1-22(2)20(30)28-19-13(34-22)6-7-16(27-19)26-18-12(23)10-24-21(29-18)25-11-8-14(31-3)17(33-5)15(9-11)32-4/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of R406 (free base)

DescriptionR406 (free base) is a potent inhibitor of Syk with IC50 of 41 nM.
TargetsSyk    
IC5041 nM     

R406 (free base) Dilution Calculator

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R406 (free base) Molarity Calculator

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Preparing Stock Solutions of R406 (free base)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1259 mL 10.6293 mL 21.2585 mL 42.517 mL 53.1463 mL
5 mM 0.4252 mL 2.1259 mL 4.2517 mL 8.5034 mL 10.6293 mL
10 mM 0.2126 mL 1.0629 mL 2.1259 mL 4.2517 mL 5.3146 mL
50 mM 0.0425 mL 0.2126 mL 0.4252 mL 0.8503 mL 1.0629 mL
100 mM 0.0213 mL 0.1063 mL 0.2126 mL 0.4252 mL 0.5315 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on R406 (free base)

R406 is a potent SYK inhibitorSpleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase mainly expressed in hematopoietic cells. It transmits signals from a variety of cell surface receptors including CD74, Fc receptor and integrins. It is crucial for adaptive immune response, and also very important for cellular adhesion, innate immune recognition, osteoclast maturation, platelet activation and vascular development. [1]

Functional abnormality of SYK has been implicated in several blood malignancies. Constitutively active SYK can transform B cells. SYK inhibition can be beneficial for patients with blood cancers and autoimmune diseases.

R406 is a potent inhibitor of IgE and IgG mediated Fc receptor activation with EC50 for degranulation of 56-64 nM. [2] R406 targets SYK and inhibits phosphorylation of SYK substrates by binding to its ATP binding pocket and competing with ATP. R406 strongly inhibits SYK kinase activity with an IC50 of 41 nM.

R406 induces apoptosis in diffuse large B-cell lymphoma cell lines. It blocks B cell receptor signaling through inhibiton of SYK autophosphorylation of Y525/Y526 and SYK-dependent phosphorylation of the B-cell linker protein. [3]

R406 can be administrated orally.

References:
[1]Mocsai A, Ruland J, Tybulewicz VL. The SYK tyrosine kinase: a crucial player in diverse biological functions. Nat Rev Immunol 2010. 10(6): 387-402.
[2]Braselmann S, Taylor V, Zhao H, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther 2006. 319(3): 998-1008.
[3]Chen L, Monti S, Juszczynski P, et al. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood 2008. 111(4): 2230*2237.

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Description

R406 free base is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.

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