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Fostamatinib disodium hexahydrate

Cat. No. M14917
Fostamatinib disodium hexahydrate Structure
Synonym:

R788 disodium hexahydrate

Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 160  USD160 In stock
50mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).

Chemical Information
Molecular Weight 732.51
CAS Number 914295-16-2
Solubility (25°C) DMSO 31.81 mg/mL
Water 2 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Ali McBride, et al. Fostamatinib disodium hexahydrate: a novel treatment for adult immune thrombocytopenia

[2] Daniel A Hussar, et al. Prucalopride succinate, Fostamatinib disodium hexahydrate, Avatrombopag maleate, and Lusutrombopag

[3] David J Sweeny, et al. Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation

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Keywords: Fostamatinib disodium hexahydrate, R788 disodium hexahydrate supplier, Syk, inhibitors, activators

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