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Submit ReviewPF 06551600 malonate is a 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.
Sold for research purposes under agreement from Pfizer Inc.
PF 06651600 malonate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 389.41 |
公式 | C15H19N5O.C3H4O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2140301-97-7 |
PubChem ID | 124203830 |
InChI Key | QMPMPSGDPRHZCG-VZXYPILPSA-N |
Smiles | C[C@H]1CC[C@@H](NC2=C3C=CNC3=NC=N2)CN1C(C=C)=O.OC(CC(O)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 38.94 | 100 | |
DMSO | 38.94 | 100 |
以下数据基于产品分子量 389.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.57 mL | 12.84 mL | 25.68 mL |
5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for PF 06551600 malonate, please let us know.
关键词: PF 06651600 malonate, PF 06651600 malonate supplier, PF06651600, malonate, JAK3, kinase, inhibitors, inhibits, potent, selective, anti-inflammatory, JAK, 6506, Tocris Bioscience
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平均评分: 5 (Based on 1 Review.)
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