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- Janus kinase (JAK)
- PF 06651600 malonate
PF 06651600 malonate
Potent and selective JAK3 inhibitor
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
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包装价格促销价数量
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5mg￥1412.001130.00- +
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25mg￥5562.004450.00- +
- 货号: ajcx27642
- CAS: 2140301-97-7
- 别名:
- 分子式: C15H19N5O.C3H4O4
- 分子量: 389.41
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
Potent and selective JAK3 inhibitor (IC50 = 33.1 μM). Exhibits no significant activity against a panel of other kinases including JAK1, JAK2 and TYK2. Inhibits phosphorylation of STAT5, induced by IL-2, IL-4, IL-7 and IL-15. Suppresses Th1 and Th17 T-cell differentiation and function in vitro. Reduces paw swelling in a rat model of arthritis and reduces disease severity in a rat EAE model.
Thorarensen et al (2017) Design of a Janus Kinase 3 (JAK3) specific inhibitor 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) allowing for the interrogation of JAK3 signaling in humans. J.Med.Chem. 60 1971 PMID:28139931 |Telliez et al (2016) Discovery of a JAK3-selective inhibitor: functional differentiation of JAK3-selective inhibition over pan-JAK or JAK1-selective inhibition. ACS Chem.Biol. 11 3442 PMID:27791347
