Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
| Molecular Weight | 443.5 |
| Formula | C23H25N9O |
| CAS Number | 1800046-95-0 |
| Solubility (25°C) | DMSO 89 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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