Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with an IC50 of 41 nM that strongly inhibits Syk but not Lyn and is 5-fold less potent against Flt3. Phase 3.

 

Brand: BCM

 

Target: FLT; Syk; Monoamine Transporter; Adenosine Receptor

 

Signaling Pathways: Angiogenesis; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors

 

In Vitro: In RA model,Fostamatinib significantly reduced inflammatory mediators such as TNFalpha,IL-1,IL-6 and IL-18, thereby reducing inflammation and bone degeneration. Fostamatinib was able to effectively inhibit BCR signaling in vivo, resulting in decreased proliferation and survival of malignant B cells and significantly prolonged survival of animals in the treatment group. Oral administration of Fostamatinib reduced immune complex-mediated inflammation in mouse models of reverse-passive Athers response and double antibody-induced arthritis.

 

Melting Point: 214° - 217°C

 

Boiling Point: 814.2±75.0 °C(Predicted)

 

Stability: Hygroscopic

 

pKa: 1.70±0.10(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)(O)O)C  

 

InChIKey: GKDRMWXFWHEQQT-UHFFFAOYSA-N  

 

InChI: InChI=1S/C23H26FN6O9P/c1-23(2)21(31)30(11-38-40(32,33)34)20-14(39-23)6-7-17(28-20)27-19-13(24)10-25-22(29-19)26-12-8-15(35-3)18(37-5)16(9-12)36-4/h6-10H,11H2,1-5H3,(H2,32,33,34)(H2,25,26,27,28,29) 

 

Attribute
[CAS No.]	901119-35-5
[EINECS]	618-473-2
[Formula]	C23H26FN6O9P
[Molecular]	580.5
[Chem Name]	[6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl dihydrogen phosphate
[Storage]	Keep in dark place. Sealed in dry, 2-8°C
[Synonym]	R788; Tavalisse，UNII-SQ8A3S5101; Fostamatinib
[Form]	White to Off-White Powder
[MDL No.]	MFCD16628163

Goods Tag