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).
| 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 |
| 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.
| Related Syk Products |
|---|
| Syk-IN-7
Syk-IN-7 is an inhibitor of spleen tyrosine kinase (SYK). |
| Syk-IN-8
Syk-IN-8 is a Syk inhibitor, with antiproliferative activity against multiple hematological tumour cells. |
| ER-27319
ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. |
| Dehydroabietinol
Dehydroabietinol is an abietane diterpenoid. Dehydroabietinol has kinase inhibition activity for spleen tyrosine kinase (SYK) with an IC50 value of 46.4 μM. Dehydroabietinol can be used for the research of immune-mediated disease. |
| Cevidoplenib dimesylate
Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. |
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