Date published: 2025-10-30

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R406 (CAS 841290-81-1)

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Alternate Names:
N4-(2,2-dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine
Application:
R406 is an IgE and IgG- mediated Fc signaling activation inhibitor
CAS Number:
841290-81-1
Purity:
≥98%
Molecular Weight:
628.63
Molecular Formula:
C22H23FN6O5•C6H6O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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R406 is an inhibitor of IgE and IgG-mediated activation of Fc receptor signaling, stopping the production/release of LTC4, cytokines, and chemokines, including TNFalpha, IL-8, and GM-CSF. R406 inhibits phosphorylation of Syk substrate linker and blocks Syk-dependent T-cell and B-cell activation. R406 significantly induces chronic lymphocytic leukemia (CLL) cell apoptosis in nurse-like cell co-cultures and blocks CCL3 and CCL4 secretion by CLL cells in response to B-cell antigen receptor (Bcr) triggering. R406 is a potent inhibitor of platelet signaling and Flt-3/Flk-2.


R406 (CAS 841290-81-1) References

  1. Immunotoxicity assessment for the novel Spleen tyrosine kinase inhibitor R406.  |  Zhu, Y., et al. 2007. Toxicol Appl Pharmacol. 221: 268-77. PMID: 17490694
  2. The novel Syk inhibitor R406 reveals mechanistic differences in the initiation of GPVI and CLEC-2 signaling in platelets.  |  Spalton, JC., et al. 2009. J Thromb Haemost. 7: 1192-9. PMID: 19422460
  3. 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. 2009. Blood. 114: 1029-37. PMID: 19491390
  4. Contribution of gut bacteria to the metabolism of the spleen tyrosine kinase (Syk) inhibitor R406 in cynomolgus monkey.  |  Sweeny, DJ., et al. 2010. Xenobiotica. 40: 415-23. PMID: 20415544
  5. The Syk-kinase inhibitor R406 impairs platelet activation and monocyte tissue factor expression triggered by heparin-PF4 complex directed antibodies.  |  Lhermusier, T., et al. 2011. J Thromb Haemost. 9: 2067-76. PMID: 21848694
  6. Pharmacokinetics and efficacy of the spleen tyrosine kinase inhibitor r406 after ocular delivery for retinoblastoma.  |  Pritchard, EM., et al. 2014. Pharm Res. 31: 3060-72. PMID: 24906597
  7. In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib.  |  Rolf, MG., et al. 2015. Pharmacol Res Perspect. 3: e00175. PMID: 26516587
  8. Syk inhibitor R406 downregulates inflammation in an in vitro model of Pseudomonas aeruginosa infection.  |  Alhazmi, A., et al. 2018. Can J Physiol Pharmacol. 96: 182-190. PMID: 29020462
  9. The Syk inhibitor R406 is a modulator of P-glycoprotein (ABCB1)-mediated multidrug resistance.  |  Duran, GE. and Sikic, BI. 2019. PLoS One. 14: e0210879. PMID: 30668583
  10. R406 elicits anti-Warburg effect via Syk-dependent and -independent mechanisms to trigger apoptosis in glioma stem cells.  |  Sun, S., et al. 2019. Cell Death Dis. 10: 358. PMID: 31043589
  11. Identification of SYK inhibitor, R406 as a novel senolytic agent.  |  Cho, HJ., et al. 2020. Aging (Albany NY). 12: 8221-8240. PMID: 32379705
  12. The effect of spleen tyrosine kinase inhibitor R406 on diabetic retinopathy in experimental diabetic rats.  |  Su, X., et al. 2020. Int Ophthalmol. 40: 2371-2383. PMID: 32462561
  13. Inhibition of Spleen Tyrosine Kinase Restores Glucocorticoid Sensitivity to Improve Steroid-Resistant Asthma.  |  Liu, Q., et al. 2022. Front Pharmacol. 13: 885053. PMID: 35600871

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

R406, 2 mg

sc-364595
2 mg
$160.00

R406, 10 mg

sc-364595A
10 mg
$370.00