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Chemical Structure| 914295-16-2 Chemical Structure| 914295-16-2

Structure of 914295-16-2

Chemical Structure| 914295-16-2

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R788 Disodium is a Syk inhibitor with IC50 of 41 nM. It is the prodrug of metabolite R406 with immunomodulatory activity.

Synonyms: R788 disodium hexahydrate; Tavalisse; Tamatinib Fosdium hexahydrate

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Product Details of Fostamatinib disodium hexahydrate

CAS No. :914295-16-2
Formula : C23H36FN6Na2O15P
M.W : 732.51
SMILES Code : O=C1N(COP([O-])([O-])=O)C2=NC(NC3=NC(NC4=CC(OC)=C(OC)C(OC)=C4)=NC=C3F)=CC=C2OC1(C)C.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Na+].[Na+]
Synonyms :
R788 disodium hexahydrate; Tavalisse; Tamatinib Fosdium hexahydrate
MDL No. :MFCD19443649
InChI Key :ZQGJCHHKJNSPMS-UHFFFAOYSA-L
Pubchem ID :24828759

Safety of Fostamatinib disodium hexahydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Related Pathways of Fostamatinib disodium hexahydrate

RTK

Isoform Comparison

Biological Activity

Description
Fostamatinib (R788) disodium hexahydrate serves as the oral prodrug of the active compound R406 [1].

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMDM) 500 nmol/L 24 hours To investigate the effect of Fostamatinib on macrophage polarization. Results showed that Fostamatinib prevented IL4-induced expression of immunosuppressive genes and downregulated the expression of these genes in macrophages cocultured with KPC1245 tumor cells. PMC10416758

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice (C57BL/6) Orthotopic pancreatic ductal adenocarcinoma (PDAC) model Intraperitoneal injection 50 mg/kg Five times per week, continuous treatment To evaluate the effect of Fostamatinib alone or in combination with gemcitabine on PDAC growth and metastasis. Results showed that Fostamatinib significantly reduced tumor growth and metastasis and remodeled the tumor immune microenvironment, enhancing CD8+ T cell responses. PMC10416758
NOD.SCID mice Xenogeneic model of EBV+ B-cell lymphoma Oral fostamatinib-containing chow Continuous administration Syk inhibition did not significantly affect solid tumor growth but resulted in tumor growth in adjacent inguinal lymph nodes PMC4008139
Mice Wild-type neonatal mice Oral 40 mg/kg body weight Every 6 hours for 8 days To evaluate the effect of SYK inhibitor fostamatinib on the lymphatic system, results showed no detectable entry of blood into the thoracic duct PMC3871239
C57BL/6J mice Ischemia/reperfusion (I/R)-induced acute lung injury model Oral 3 g/kg Once daily for 10 days To evaluate the effect of Fostamatinib (R788) on MUC1 levels in a model of acute lung injury. Results showed that Fostamatinib significantly reduced MUC1 abundance in lung epithelial cells. PMC7691435
Apoe-/- mice High cholesterol diet-induced atherosclerosis model Dietary administration 0.3% (w/w) Continuous for 8 or 20 weeks Evaluate the effect of Fostamatinib on early and late-stage atherosclerosis. Results showed Fostamatinib significantly reduced plaque size and macrophage accumulation in early lesions but had limited effect in late-stage lesions. PMC4759214
NOD/SCID gamma mice Subcutaneous xenograft model Intraperitoneal injection 40 mg/kg and 80 mg/kg Daily administration for 33 days To evaluate the inhibitory effect of Fostamatinib on xenograft tumor growth. PMC6009761

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.37mL

0.27mL

0.14mL

6.83mL

1.37mL

0.68mL

13.65mL

2.73mL

1.37mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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