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Fostamatinib (R788)

Cat. No. M1990
Fostamatinib (R788) Structure
Synonym:

Fostamatinib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 76  USD76 In stock
10mg USD 110  USD110 In stock
50mg USD 330  USD330 In stock
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Quality Control
Biological Activity

Fostamatinib (R788) is a prodrug of the active compound tamatinib (R-406), which is an inhibitor of the enzyme spleen tyrosine kinase (Syk). R788 (Fostamatinib) effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals. R788 also inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8 and GM-CSF. R788 (Fostamatinib) induces apoptosis of the majority of examined DLBCL cell lines. Fostamatinib is orally bioavailable and was well tolerated in phase I and II trials, with the most common side effect being gastrointestinal symptoms. Fostamatinib is currently in phase III clinical trials for rheumatoid arthritis and phase II trials for autoimmune thrombocytopenia and lymphoma.

Customer Product Validations & Biological Datas
Source Blood (2010). Figure 2.R788
Method apoptosis assay
Cell Lines TCL1 leukemia cells
Concentrations 10 μM
Incubation Time 24, 48, and 72 h
Results As shown in Figure 2, a modest decrease in the percentage of viable (annexin V/PI negative) cells was observed at the highest R406 concentrations.
Protocol
Cell Experiment
Cell lines Cultured human mast cells (CHMC)
Preparation method Human Mast Cell Culture and Stimulation.
Cultured human mast cells (CHMC) were derived from cord blood CD34+ progenitor cells and grown, primed, and stimulated as described previously (Rossi et al., 2006) and shown in supplemental data. Before stimulation, cells were incubated with R406 or DMSO for 30 min. Cells were then stimulated with either 0.25 to 2 mg/ml anti-IgE or anti-IgG or 2 μM ionomycin. For tryptase measurement, ∼1500 cells per well were stimulated for 30 min in modified Tyrode's buffer. For LTC4 and cytokine production, 100,000 cells per well were stimulated for 1 or 7 h, respectively. Tryptase activity was measured by luminescence readout of a peptide substrate, and LTC4 and cytokines were measured using Luminex multiplex technology.
Concentrations 0~20 μM
Incubation time 30 min
Animal Experiment
Animal models K/BxN Model Arthritis induced in C57BL/6 mice
Formulation 35% TPGS, 60% PEG 400, and 5% propylene glycol
Dosages 5 and 10mg/kg b.i.d for 13 days
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 580.46
Formula C23H26FN6O9P
CAS Number 901119-35-5
Purity 99.55%
Solubility DMSO 96 mg/mL
Storage at -20°C
References

[1] Suljagic M, et al. Blood. The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Eμ- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling.

[2] Bajpai M. IDrugs. Fostamatinib, a Syk inhibitor prodrug for the treatment of inflammatory diseases.

[3] Braselmann S, et al. J Pharmacol Exp Ther. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.

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Keywords: Fostamatinib (R788), Fostamatinib supplier, Syk, inhibitors

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