| Hazard Information | Back Directory | [Description]
TAS05567 is a potent and selective orally available Syk inhibitor, which inhibits BCR-dependent cell signaling as well as FcR-mediated immune responses. | [Uses]
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[1]. | [in vivo]
TAS05567 (10-30 mg/kg; oral administration; daily; for 9 days; female BALB/c mice) treatment suppresses hind-paw swelling in a dose-dependent manner. The serum MMP-3 levels are significantly lower in both the 10 mg/kg and 30 mg/kg TAS05567 groups than in the vehicle group[1]. | Animal Model: | Female BALB/c mice (7-8 weeks old) injected with collagen antibody[1] | | Dosage: | 10 mg/kg, 30 mg/kg | | Administration: | Oral administration; daily; for 9 days | | Result: | Suppressed hind-paw swelling in a dose-dependent manner.
|
| [References]
[1] Hayashi H, et al. TAS05567, a Novel Potent and Selective Spleen Tyrosine Kinase Inhibitor, Abrogates Immunoglobulin-Mediated Autoimmune and Allergic Reactions in Rodent Models. J Pharmacol Exp Ther. 2018 Jul;366(1):84-95. DOI:10.1124/jpet.118.248153 |
|
|