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505819 Syk Inhibitor VI, R406 - CAS 841290-80-0 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N⁴-(2,2-Dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N²-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, 6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one

Primary Target: Syk kinase
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Replacement Information

Tabulka spec. kláve

CAS #Empirical Formula
841290-80-0C₂₂H₂₃FN₆O₅
Description
OverviewA cell-permeable, orally bioavailable pyrimidinediamino compound with anti-inflammatory and anti-tumor properties. Acts as a potent, reversible and ATP-competitive inhibitor of Syk kinase (IC50 = 41 nM; Ki = 30 nM). Exhibits high selectivity over a broad panel of other protein kinases (˜300 nM), ion channels, and enzymes. Blocks Syk-dependent FcR-mediated activation of monocytes/macrophages, and neutrophils and inhibits Anti-IgE-mediated degranulation in cultured human mast cells (EC50 = 56 nM as measured by tryptase release). At higher concentrations, it is shown to block adenosine A3 receptors, adenosine transporter, and monoamine transporter (IC50 = 81 nM, 1.84 µM, and 2.74 µM, respectively), and Flt3 autophosphorylation. Shown to reduce immune complex-mediated inflammation in murine models (˜10 mg/kg) and diminish airway hyper-responsiveness in asthma models.
Catalogue Number505819
Brand Family Calbiochem®
SynonymsN⁴-(2,2-Dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N²-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, 6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
References
ReferencesFriedberg, J.W., et al. 2010. Blood 115, 2578.
Young, R.M., et al. 2009. Blood 113, 2508.
Young, R.M., et al. 2009. Blood 113, 2508.
Chen, L., et al. 2008. Blood 111, 2230.
Braselmann, S., et al. 2006. J. Pharmacol. Exp. Ther. 319, 998.
Product Information
CAS number841290-80-0
FormOff-white powder
Hill FormulaC₂₂H₂₃FN₆O₅
Chemical formulaC₂₂H₂₃FN₆O₅
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetSyk kinase
Primary Target K<sub>i</sub>30 nM)
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalogové číslo GTIN
505819 0

Documentation

Syk Inhibitor VI, R406 - CAS 841290-80-0 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
Friedberg, J.W., et al. 2010. Blood 115, 2578.
Young, R.M., et al. 2009. Blood 113, 2508.
Young, R.M., et al. 2009. Blood 113, 2508.
Chen, L., et al. 2008. Blood 111, 2230.
Braselmann, S., et al. 2006. J. Pharmacol. Exp. Ther. 319, 998.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision27-September-2013 JSW
SynonymsN⁴-(2,2-Dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N²-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, 6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
DescriptionA cell-permeable, orally bioavailable pyrimidinediamino compound with anti-inflammatory and anti-tumor properties. Acts as a potent, reversible and ATP-competitive inhibitor of Syk kinase (IC50 = 41 nM; Ki = 30 nM). Exhibits high selectivity over a broad panel of other protein kinases (˜300 nM), ion channels, and enzymes. Blocks Syk-dependent FcR-mediated activation of monocytes/macrophages, and neutrophils and inhibits Anti-IgE-mediated degranulation in cultured human mast cells (EC50 = 56 nM as measured by tryptase release). At higher concentrations, it is shown to block adenosine A3 receptors, adenosine transporter, and monoamine transporter (IC50 = 81 nM, 1.84 µM, and 2.74 µM, respectively), and Flt3 autophosphorylation. Shown to reduce immune complex-mediated inflammation in murine models (˜10 mg/kg) and diminish airway hyper-responsiveness in asthma models.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number841290-80-0
Chemical formulaC₂₂H₂₃FN₆O₅
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesFriedberg, J.W., et al. 2010. Blood 115, 2578.
Young, R.M., et al. 2009. Blood 113, 2508.
Young, R.M., et al. 2009. Blood 113, 2508.
Chen, L., et al. 2008. Blood 111, 2230.
Braselmann, S., et al. 2006. J. Pharmacol. Exp. Ther. 319, 998.