RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.
| Molecular Weight | 355.44 |
| Formula | C18H25N7O |
| CAS Number | 1446790-62-0 |
| Solubility (25°C) | DMSO 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 |
|---|
| 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. |
| Cevidoplenib
Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. |
| Syk-IN-1
Syk-IN-1 (compound 4) is a potent Syk inhibitor, with an IC50 of 35 nM. |
| TAS05567
TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases. |
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