Tofacitinib . citrate
| Code | Size | Price |
|---|
| CDX-T0461-M005 | 5 mg | £67.00 |
Quantity:
| CDX-T0461-M025 | 25 mg | £240.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Documents
Further Information
Alternate Names/Synonyms:
CP-690550; Xeljanz; Tasocitinib; (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-beta-oxo-1-piperidinepropanenitrile citrate salt
Appearance:
White to off-white powder.
CAS:
540737-29-9
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Protect from light and moisture.
InChi:
InChI=1S/C16H20N6O.C6H8O7/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16;7-3(8)1-6(13,5(11)12)2-4(9)10/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t11-,13+;/m1./s1
InChiKey:
SYIKUFDOYJFGBQ-YLAFAASESA-N
Long Description:
Chemical. CAS: 540737-29-9. Formula: C16H20N6O . C6H8O7. MW: 312.4 . 192.1. Synthetic. 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.
MDL:
MFCD11616529
Molecular Formula:
C16H20N6O . C6H8O7
Molecular Weight:
312.4 . 192.1
Package Type:
Vial
Product Description:
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. It is investigated against the spread of the SARS-CoV-2 (COVID-19).
Purity:
>98% (HPLC)
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
Solubility Chemicals:
Soluble in DMSO (20mg/ml) or DMF (5 mg/ml). Slightly soluble in ethanol.
Source / Host:
Synthetic
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at RT.
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)