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Fostamatinib

CAS No.
901119-35-5
Chemical Name:
Fostamatinib
Synonyms
R788;RT788;CS-883;R7935788;R-935788;R788 5MG;NSC-745942;Tavalisse);Fostatinib;R788, >=99%
CBNumber:
CB52499223
Molecular Formula:
C23H26FN6O9P
Molecular Weight:
580.46
MDL Number:
MFCD16628163
MOL File:
901119-35-5.mol
Last updated:2024-11-21 18:03:03

Fostamatinib Properties

Melting point 214° - 217°C
Boiling point 814.2±75.0 °C(Predicted)
Density 1.496
storage temp. -20°C, Hygroscopic
solubility DMSO (Slightly), Methanol (Slightly)
pka 1.70±0.10(Predicted)
form Solid
color White to Off-White
Stability Hygroscopic
NCI Dictionary of Cancer Terms fostamatinib disodium
FDA UNII SQ8A3S5101
NCI Drug Dictionary fostamatinib disodium
ATC code B02BX09

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P280-P305+P351+P338

Fostamatinib price More Price(25)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Usbiological 474099 Fostamatinib 901119-35-5 100mg $1423 2021-12-16 Buy
Matrix Scientific 125210 Fostamatinib 95+% 901119-35-5 1g $3036 2021-12-16 Buy
ChemScene CS-2152 Fostamatinib 99.20% 901119-35-5 100mg $708 2021-12-16 Buy
ApexBio Technology B2284 Fostamatinib(R788) 901119-35-5 100mg $713 2021-12-16 Buy
AK Scientific X2110 Fostamatinibdisodium 901119-35-5 1g $4148 2021-12-16 Buy
Product number Packaging Price Buy
474099 100mg $1423 Buy
125210 1g $3036 Buy
CS-2152 100mg $708 Buy
B2284 100mg $713 Buy
X2110 1g $4148 Buy

Fostamatinib Chemical Properties,Uses,Production

Binding Mode

As shown in the co-crystal structure of tamatinib-SYK (Fig. 1), the aminopyrimidine moiety forms two hydrogen bonds with Ala451 of the hinge region. In addition, there is an atypical hydrogen bond (CH...O=C) between CH at 6 and amide carbonyl of Glu449 (Fig. 2).
Figure 1. Co-crystal structure of tamatinib (parent  drug of fostamatinib) with SYK (PDB ID: 3FQS).Figure 2. Summary of tamatinib–SYK interactions  based on their co-crystal structure

Uses

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

Indications

Fostamatinib is an FDA-approved first-in-class spleen tyrosine kinase (SYK) inhibitor, specifically indicated for the treatment of adult patients with chronic immune thrombocytopenia (ITP) who have not responded adequately to prior therapies.

brand name

Tavalisse

General Description

Class: non-receptor tyrosine kinase; Treatment: ITP; Other name: R788; Oral bioavailability = 100% (prodrug); Elimination half-life = 15 h (tamatinib); Protein binding = 98.3%

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].

target

Primary target: SYK

References

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

901119-38-8
901119-35-5
Synthesis of Fostamatinib from Ditert-butyl [6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxo-pyrido[3,2-b][1,4]oxazin-4-yl]methyl phosphate
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  • Fostamatinib is an inhibitor of spleen tyrosine kinase (SYK), a key regulator of signal transduction pathways involved in vari....
  • Dec 26,2023

View Lastest Price from Fostamatinib manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Fostamatinib (R788) pictures 2024-11-25 Fostamatinib (R788)
901119-35-5
US $0.00-0.00 / g 10g 99% HPLC 1000kg HangZhou RunYan Pharma Technology Co.,LTD.
Fostamatinib pictures 2024-11-22 Fostamatinib
901119-35-5
US $0.00 / g 1g 98%min 1000g WUHAN FORTUNA CHEMICAL CO., LTD
Fostamatinib pictures 2024-11-19 Fostamatinib
901119-35-5
US $36.00-81.00 / mg 98.3% 10g TargetMol Chemicals Inc.
  • Fostamatinib (R788) pictures
  • Fostamatinib (R788)
    901119-35-5
  • US $0.00-0.00 / g
  • 99% HPLC
  • HangZhou RunYan Pharma Technology Co.,LTD.
  • Fostamatinib pictures
  • Fostamatinib
    901119-35-5
  • US $0.00 / g
  • 98%min
  • WUHAN FORTUNA CHEMICAL CO., LTD
  • Fostamatinib pictures
  • Fostamatinib
    901119-35-5
  • US $36.00-81.00 / mg
  • 98.3%
  • TargetMol Chemicals Inc.

Fostamatinib Spectrum

Fostamatinib FostaMatinib DisodiuM FostaMatinib (R788) 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 R788, >=99% FOSTAMATINIB (R788);R788 R788 5MG Tavalisse) {[6-({5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]py rimidin-4-yl}amino)-2,2-dimethyl-3-oxo-2H,3H,4H- pyrido[3,2-b][1,4]oxazin-4-yl]methoxy}phosphonic acid sodium (6-((5-fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)methyl phosphate Fostamatinib USP/EP/BP 2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one, 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]- R788 free base R788 (Fostamatinib, FosD, tamatinib fosdium) CS-883 R 788;R-788;R788 [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 RT788 Blessing him Fostatinib 13C,2H3]-Fostamatinib (6-((5-Fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl dihydrogen phosphate?, Fostamatinib (6-((5-Fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl dihydrogen phosphate 901119-35-5 C23H26FN6O9P Inhibitors API