TAS05567
作者：齐岳
发布时间：2023-09-07
09:26:06
点击数：
产品名称：TAS05567
产品描述：
| 产品描述 | 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. |
| 靶点活性 | JAK2:4.8 nM, FLT3:10 nM, KDR:600 nM, Syk:0.37 nM, RET:29 nM |
| 体外活性 | 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]. |
| 体内活性 | 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]. |
| 分子量 | 439.51 |
| 分子式 | C21H29N9O2 |
| CAS No. | 1429038-15-2 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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