901119-35-5

Basic information

• Product Name: Fostamatinib
• Synonyms: Fostamatinib;FostaMatinib DisodiuM;FostaMatinib (R788);NSC-745942;R-935788;R7935788;6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one;(6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2,3-dihydropyrido[3,2-b][1,4]oxazin-4-yl)methyl dihydrogen phosphate
• CAS NO: 901119-35-5
• Molecular Formula: C₂₃H₂₆FN₆O₉P
• Molecular Weight: 580.4595042
• EINECS: 1533716-785-6
• Product Categories: Inhibitors
• Mol File: 901119-35-5.mol
• Article Data: 6

Chemical Properties

• Boiling Point: 814.248 °C at 760 mmHg
• Flash Point: 446.242 °C
• Appearance: /
• Density: 1.496
• Storage Temp.: -20°C, Hygroscopic
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 1.70±0.10(Predicted)
• Stability: Hygroscopic
• CAS DataBase Reference: Fostamatinib(CAS DataBase Reference)
• NIST Chemistry Reference: Fostamatinib(901119-35-5)
• EPA Substance Registry System: Fostamatinib(901119-35-5)

Safety Data

• Hazardous Substances Data: 901119-35-5(Hazardous Substances Data)

Usage

Uses

Fostamatinib can be used to treat cancers that have acquired resistance to kinase inhibitors.

Biological Activity

fostamatinib is a small molecule inhibitor of spleen tyrosine kinase (syk) with ic50 value of 41nm [1].fostamatinib is an orally bioavailable prodrug of r406. it is developed for the treatment of autoimmune diseases. the effective metabolite of fostamatinib, r406, is an atp-competitive inhibitor of syk with ki value of 30nm. r406 also inhibits the activity of other kinases including flt3, lyn (ic50=63nm) and lck (ic50=37nm). it is found that r406 inhibits both bcr and fcr mediated responses in vitro. besides that, r406 also shows effects in other cells types and signalling pathways. in the in vivo assay, fostamatinib shows to be highly active to inhibit fcr-mediated signaling in various animal models of allergy, autoimmunity and inflammation. moreover, fostamatinib also exerts efficacy in sle animal models. treatment of fostamatinib suppresses the established renal and skin disease and reduces lymphadenopathy in the mrl/lpr strain [1].

references

[1] mcadoo s p, tam f w k. fostamatinib disodium. drugs of the future, 2011, 36(4): 273.

Upstream product

• 118-90-1 ortho-methylbenzoic acid 
• 108-44-1 1-amino-3-methylbenzene 
• 901119-38-8 N₄-(2,2-dimethyl-4-[(di-tert-butyl-phosphonoxy)methyl]-3-oxo-5-pyrido[1,4]oxazin-6-yl)-5-fluoro-N₂-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine 
• 933-88-0 ortho-toluoyl chloride 
• 841290-80-0 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one 

Relevant articles and documents

METHOD OF BLOCKING OR AMELIORATING CYTOKINE RELEASE SYNDROME

Disclosed herein are embodiments of a method for treating or preventing cytokine release syndrome (CRS). In certain embodiments, the method comprises administering a compound, or a salt, solvate, prodrug or pharmaceutical composition thereof, to a subject experiencing, or at risk of developing, CRS. The compound may be a Syk inhibitor, and/or may have a structure according to Formula I. And the method may comprise administering the compound to a subject who is has received, is currently receiving, and/or will be receiving a cell therapy.

Methods of Treating Cell Proliferative Disorders

The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a RET kinase inhibitor. Cell proliferative disorders treatable by the methods include, thyroid tumors.

PROCESS FOR PREPARING BENZAZEPINE COMPOUNDS OR SALTS THEREOF

This invention provides a process for preparing benzazepine compounds of the formula (1): wherein X1is a halogen atom, R1and R2are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.