Specifications
- Purity
- ≥98% (HPLC)
- Appearance
- White to off-white powder
- Identity
- 1H-NMR
Properties
- Solvents
- DMSO (20 mg/ml), DMF (5 mg/ml), ethanol (slightly)
- Melting Point
- 198-202° C (dec.)
Category: API's & Intermediates
Tofacitinib citrate is a potent cell permeable JAK3 inhibitor (IC50=1nM), which Shows also JAK-1 inhibitory activity. This is an immunosuppressive and anti-inflammatory agent. It inhibits signaling through heterodimeric receptors associated with JAK3, JAK1, or both of them, with functional selectivity over JAK2-paired receptors. Blocks downstream STAT signaling, resulting in potent inhibition of several cytokines, including interleukins 2, 4, 7, 9, 15 and 21, which are integral to lymphocyte activation, function and proliferation. It also has been shown to be a potent and selective inhibitor of HIV-1 replication and virus reactivation in vitro.
Synonyms | CP-690550, Xeljanz, Tasocitinib, (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-ß-oxo-1-piperidinepropanenitrile citrate salt |
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Purity | ≥98% (HPLC) |
Appearance | White to off-white powder |
CAS-Number | 540737-29-9 |
Molecular Formula | C16H20N6O · C6H8O7 |
Molecular Weight | 504.49 |
Identity | 1H-NMR |
Solvents | DMSO (20 mg/ml), DMF (5 mg/ml), ethanol (slightly) |
Melting Point | 198-202° C (dec.) |
Smiles | OC(CC(O)=O)(CC(O)=O)C(O)=O.O=C(CC#N)N1C[C@@H]([C@H](C)CC1)N(C)C2=NC=NC3=C2C=CN3 |
InChi Key | SYIKUFDOYJFGBQ-YLAFAASESA-N |
Shipping | AMBIENT |
Short Term Storage | RT |
Long Term Storage | RT |
Handling Advice | Protect from light and moisture. |
Use / Stability | Stable for at least 2 years after receipt when stored at RT. |
Transportation | Not dangerous goods |
References | (1) P.S. Changelian, et al., Science 302, 875 (2003), (2) D.C. Borie, et al., Transplantation 79, 791 (2005), (3) D.C. Borie, et al., Transplantation 80, 1756 (2005), (4) K. West, Curr. Opin. Investig. Drugs 10, 491 (2009) (Review), (5) M.E. Flanagan, et al., J. Med. Chem. 53, 8468 (2010), (6) W. Ju, et al., Blood 117, 1938 (2011), (7) C. Gavegnano, et al., Antimicrob. Agents Chemother. 58, 1977 (2014), (8) S.P. Wang, et al., Ann. Rheum. Dis. 73, 2213 (2014) |
Quantity | 5 mg, 25 mg, Bulk |