Sovalleplenib is a potent, orally active, selective Syk inhibitor with an IC50 of 25 nM.Sovalleplenib inhibits tyrosine kinase-dependent Fcγ receptor-mediated phagocytosis by macrophages, which in turn reduces phagocytotic destruction of platelets, as well as reduces production of antiplatelet antibodies by B-cells.Sovalleplenib has antitumor activity in immune thrombocytopenia (ITP).
| Molecular Weight | 482.60 |
| Formula | C24H30N6O3S |
| CAS Number | 1415792-84-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 25 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 |
|---|
| Syk Kinase Peptide Substrate
Syk Kinase Peptide Substrate is a Syk kinase peptide substrate. |
| TOP1288
TOP1288 is an SRC/Syk/p38α inhibitor for studies related to ulcerative colitis. |
| R343
R343 is an immunoglobulin E (IgE) as well as spleen tyrosine kinase (Syk) inhibitor for studies related to allergic asthma and non-small cell lung cancer. |
| R333
R333 is a JAK/SYK inhibitor that can be used in studies related to discoid lupus erythematosus (DLE). |
| PRT2761
PRT2761 is a spleen tyrosine kinase (Syk) inhibitor that may be used in studies related to allergic conjunctivitis. |
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