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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $2,270 | 10-14 weeks | |
50 mg | $2,980 | 10-14 weeks | |
100 mg | $4,000 | 10-14 weeks |
Description | TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM), showing >70% inhibition of Syk and four other kinases [FLT3 (IC50: 10 nM), JAK2 (IC50: 4.8 nM), KDR (IC50: 600 nM), RET (IC50: 29 nM)] in a panel of 192 kinases. |
Targets&IC50 | JAK2:4.8 nM, FLT3:10 nM, KDR:600 nM, RET:29 nM, Syk:0.37 nM |
In vitro | TAS05567 inhibits PLCγ2 (IC50: 23 nM) and Erk1/2 (IC50: 9.8 nM), after stimulation of Ramos cells with anti-IgM. TAS05567 inhibits the formation of mature osteoclasts in a concentration-dependent manner, and osteoclast differentiation is completely suppressed at 30 nM. TAS05567 suppresses both calcium flux (IC50: 27 nM) and histamine release (IC50: 13 nM) induced by cross-linking of FcεRI with IgE and antigen. TAS05567 shows concentration-dependent inhibition of TNF-α production by THP-1 cells stimulated with IgG. When Ramos cells are pretreated with TAS05567 prior to BCR cross-linking by exposure to anti-IgM, there is marked inhibition of the phosphorylation of BLNK. The IC50 of TAS05567 for suppressing the induction of BLNK phosphorylation by anti-IgM is 1.8 nM [1]. |
In vivo | TAS05567 (10-30 mg/kg; p.o.; daily; for 9 days; female BALB/c mice) treatment inhibits hind-paw swelling dose-dependently, and significantly reduces serum MMP-3 levels at both 10 mg/kg and 30 mg/kg compared to the vehicle group [1]. |
Molecular Weight | 439.51 |
Formula | C21H29N9O2 |
Cas No. | 1429038-15-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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