505819 Sigma-AldrichSyk Inhibitor VI, R406 - CAS 841290-80-0 - Calbiochem

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

SDS
References
Data Sheet

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

Recommended Products

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₂₃FN₆O₅

Pricing & Availability

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Description
Overview	A 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; K_i = 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 Number	505819
Brand Family	Calbiochem®
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

References
References	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.

Product Information
CAS number	841290-80-0
Form	Off-white powder
Hill Formula	C₂₂H₂₃FN₆O₅
Chemical formula	C₂₂H₂₃FN₆O₅
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	Syk kinase
Primary Target K<sub>i</sub>	30 nM)
Purity	≥99% by HPLC

Physicochemical Information
Cell permeable	Y

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 Instructions	Following 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

Documentation

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

Title
Safety Data Sheet (SDS)

References

Reference overview
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.

Revision	27-September-2013 JSW
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
Description	A 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; K_i = 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.
Form	Off-white powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	841290-80-0
Chemical formula	C₂₂H₂₃FN₆O₅
Structure formula
Purity	≥99% by HPLC
Solubility	DMSO (25 mg/ml)
Storage	+2°C to +8°C Protect from light
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	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.