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Submit ReviewCP 690550 citrate is a potent JAK inhibitor (IC50 values are 1, 20, and 112 nM for JAK3, JAK2 and JAK1 respectively). Orally active immunosuppressant; exhibits efficacy in rodent rheumatoid arthritis models.
Sold for research purposes under agreement from Pfizer Inc.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of CP 690550 (Tofacitinib) is reviewed on the chemical probes website.
CP 690550 citrate is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library, Tocriscreen Epigenetics Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 504.49 |
公式 | C16H20N6O.C6H8O7 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 540737-29-9 |
PubChem ID | 10174505 |
InChI Key | SYIKUFDOYJFGBQ-YLAFAASESA-N |
Smiles | C[C@H]1[C@@H](N(C2=NC=NC3=C2C=CN3)C)CN(C(CC#N)=O)CC1.OC(CC(O)=O)(C(O)=O)CC(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 | |||
DMSO | 50.45 | 100 |
以下数据基于产品分子量 504.49。 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 | 1.98 mL | 9.91 mL | 19.82 mL |
5 mM | 0.4 mL | 1.98 mL | 3.96 mL |
10 mM | 0.2 mL | 0.99 mL | 1.98 mL |
50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
参考文献是支持产品生物活性的出版物。
Jiang et al (2008) Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J.Med.Chem. 51 8012 PMID: 19053756
Flanagan et al (2010) Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. J.Med.Chem. 53 8468 PMID: 21105711
Dowty et al (2013) Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis. J.Pharmacol.Exp.Ther. 348 165 PMID: 24218541
If you know of a relevant reference for CP 690550 citrate, please let us know.
关键词: CP 690550 citrate, CP 690550 citrate supplier, CP690550, immunosuppressants, autoimmune, antirheumatics, rheumatoid, arthritis, pfizer, JAK, janus, kinase, JAK1, JAK2, JAK3, inhibitors, inhibits, Tofacitinib, citrate, Kinase, 4556, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CP 690550 citrate 的部分引用包括:
Chin Wai et al (2022) Interleukins 4 and 21 Protect Anti-IgM Induced Cell Death in Ramos B Cells: Implication for Autoimmune Diseases. Front Immunol 13 919854 PMID: 35911775
Tetsuro et al (2020) Targeted therapy guided by single-cell transcriptomic analysis in drug-induced hypersensitivity syndrome: a case report. Nat Med 26 236-243 PMID: 31959990
Yu et al (2017) PLCγ-dependent mTOR signalling controls IL-7-mediated early B cell development. Nat Commun 8 1457 PMID: 29133930
Zhu et al (2015) Adenosine 5'-monophosphate-activated protein kinase regulates IL-10-mediated anti-inflammatory signaling pathways in macrophages. Nat Commun 194 584 PMID: 25512602
Tactacan et al (2015) The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling. Mol Cancer 14 139 PMID: 26215634
Eun-Kyoung et al (2017) The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells. Int J Mol Sci 18 PMID: 29077055
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平均评分: 5 (Based on 1 Review.)
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