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TAS05567

Catalog No. T16995 CAS 1429038-15-2

TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). 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) in a panel of 192 kinases.

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TAS05567, CAS 1429038-15-2

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). 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) in a panel of 192 kinases.
Targets&IC50	FLT3:10 nM, JAK2:4.8 nM, KDR:600 nM, Syk:0.37 nM, RET:29 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 in a dose-dependent manner. The serum MMP-3 levels are obviously lower in both the 10 mg/kg and 30 mg/kg TAS05567 groups than in 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 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TAS05567 1429038-15-2 JAK/STAT信号通路表观遗传蛋白酪氨酸激酶凋亡干细胞血管生成 c-RET JAK FLT Syk TAS-05567 Inhibitor inhibitor inhibit

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