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Ruxolitinib
- INCB 018424 phosphate
- Parent CAS: 941678-49-5
- Optical Purity: 98% e.e.
- Soluble in water and DMSO
- MF: C17H18N6.H3O4P
- MW: 404.36
Description
Ruxolitinib is an orally bioavailable JAK1/JAK2 inhibitor with reported IC50 values of 2.7 nM for JAK1 and 4.5 nM for JAK2.
JAK1 and JAK2 transmit cytokine and growth-factor signals through STAT transcription factors. Ruxolitinib is a benchmark compound for studying JAK-STAT pathway inhibition in myeloproliferative neoplasm, inflammatory and immune signaling models.
Key Features
- Potent JAK1 and JAK2 inhibitor
- Reported IC50: 2.7 nM for JAK1 and 4.5 nM for JAK2
- Blocks cytokine-driven JAK-STAT signaling
- Reference compound for myeloproliferative and inflammatory pathway research
Applications
- JAK kinase assays
- JAK-STAT signaling studies
- Myelofibrosis and myeloproliferative models
- Cytokine and immune signaling research
More Information
| Parent CAS No. | 941678-49-5 |
|---|---|
| Chemical Name | (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate |
| SMILES | N1C(C2C=NN([C@H](CC#N)C3CCCC3)C=2)=C2C=CNC2=NC=1.P(O)(O)(O)=O |&1:6,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C17H18N6.H3O4P/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16;1-5(2,3)4/h6,8-12,15H,1-5H2,(H,19,20,21);(H3,1,2,3,4)/t15-;/m1./s1 |
| InChiKey | JFMWPOCYMYGEDM-XFULWGLBSA-N |
| CID | 25127112 |
| Short Description | JAK1/2 inhibitor |
References
- RA Mesa. Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis. IDrugs. 2010, 13(6), 394-403.
- C Campas-Moya. Ruxolitinib. Drugs Fut. 2010, 35(6), 457.
- S Verstovsek et al. Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis. N. Engl. J. Med. 2010, 363(12), 1117-1127.
- A Quintas-Cardama et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 2010, 115(15), 3109-3117.
- E Apostolidou et al. JAK2 inhibitors: a reality? a hope? Clin. Lymp Myel. 2009, 9(Suppl. 3), S340-S345.
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