Fostamatinib

Fostamatinib (R788) is the oral proagent of the active compound R406[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM[2]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) [3].

Product Specifications

CAS Number

[901119-35-5]

Product Name Alternative

R788

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

FLT3; Syk

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/r788.html

Purity

99.70

Solubility

DMSO : 62.5 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O)(O)=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC

Molecular Formula

C23H26FN6O9P

Molecular Weight

580.46

Precautions

H302, H315, H319, H335

References & Citations

[1]Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36 (4) :273.|[2]Sylvia Braselmann, 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 Dec;319 (3) :998-1008.|[3]Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317 (2) :571-8.