What is the Tofacitinib citrate?

Tofacitinib citrate is , while it's Molecular Formula is C16H20N6O·C6H8O7. Tofacitinib citrate has been used:as a ligand for human serum albumin in fluorescence quenching, dynamic light scattering (DLS) measurements, differential scanning calorimetry and molecular docking studiesas a medium supplement for full depth articular cartilage (FDC) explants to monitor cytokine-induced proteoglycan lossas a Janus kinase inhibitor in MCF7 breast cancer cells

What is the CAS number for Tofacitinib citrate?

The CAS number of Tofacitinib citrate is 540737-29-9.

What is Tofacitinib citrate (540737-29-9) used for?

Tofacitinib citrate is a king of drugs developed by the US pharmaceutical company Pfizer for treating rheumatoid arthritis, trade name Xeljanz, for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid arthritis (RA) in adult patients. This product is a Janus kinase inhibitor, administered twice daily.November 6, 2012, the US Food and Drug Administration (FDA) and Pfizer jointly announced Tofacitinib citrate is approved for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid joints arthritis (RA) in adult patients.Xeljanz can be used as monotherapy or in combination with methotrexate or other non-biological disease-modifying antirheumatic drugs (the DMARD) in combination. This medicine should not be in combination with biological DMARD or strong immunosuppressants (such as cyclosporine and azathioprine). Xeljanz is approved by the daily dose of 2 times, each time 5mg.Seven clinical trials evaluated the safety and efficacy of Tofacitinib citrate in moderate to severe active RA in adult patients. In all tests, compared with patients receiving placebo, patients receiving Xeljanz treatment showed significant improvement in clinical response and physical function.In Clinical trials, the most common adverse events were upper respiratory tract infection, headache, diarrhea, nasal congestion, sore throat, and nasopharyngitis.Using Xeljanz was associated with an increased risk of serious infections, including opportunistic infections, tuberculosis, cancer and lymphoma. Xeljanz product label attaches boxed warning on these security risks. Xeljanz treatment is also associated with reducing blood cell counts and increasing cholesterol and liver enzyme values.In order to study Xeljanz long-term impact on heart disease, cancer and severe infections, FDA requires for a post-marketing study, which will evaluate two doses of Xeljanz (Tofacitinib citrate) therapy, and accept a integration of another group of patients approved by the treatment as a control.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

Product Class

540737-29-9

Product Name：Tofacitinib Citrate
Molecular Formula：C₁₆H₂₀N₆O·C₆H₈O₇
Purity：99%
Molecular Weight：504.50

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Product Details:

CasNo： 540737-29-9

Molecular Formula： C₁₆H₂₀N₆O·C₆H₈O₇

Quality Factory Supply Tofacitinib Citrate,Sale 540737-29-9 Fast Delivery

Molecular Formula:C16H20N6O·C6H8O7
Molecular Weight:504.50
Melting Point:201 °C (decomp)
Boiling Point:585.8 °C at 760 mmHg
Flash Point:308.1 °C
PSA：221.04000
LogP:0.23418

Tofacitinib citrate(Cas 540737-29-9) Usage

Description	Tofacitinib Citrate is the citrate salt obtained by combining equimolar amounts of tofacitinib, a Janus kinase (JAK) inhibitor, and citric acid. Tofacitinib is available in pill form, taken either as 5 mg twice a day (Xeljanz) or as 11 mg once per day (Xeljanz XR). It acts as a potent inhibitor of the JAK pathway, which plays a crucial role in the inflammatory response.
Chemical Structure	Tofacitinib citrate is a potent inhibitor of Janus kinase 3 (JAK3) with some JAK-1 inhibitory activity.
Uses	The brand name for Tofacitinib Citrate is XELJANZ. It was the first FDA-approved pill of its kind, belonging to the class of JAK inhibitors, for the treatment of moderate to severe rheumatoid arthritis, active psoriatic arthritis, active ankylosing spondylitis, and moderate to severe ulcerative colitis in adults. XELJANZ is available in various formulations, including immediate-release and extended-release tablets, to accommodate different dosing regimens and patient preferences.
Definition	ChEBI: A citrate salt obtained by combining equimolar amounts of tofacitinib and citric acid. Used to treat moderately to severely active Rheumatoid Arthritis.

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

540737-29-9 Relevant articles

Development of a robust, environmentally responsible process for the manufacture of tofacitinib citrate

R Vaidyanathan

Scalable Green Chemistry: Case Studies from the Pharmaceutical Industry

Process development efforts that resulted in a robust, environmentally responsible, commercializable process for tofacitinib citrate will be presented in this chapter.

Safety and efficacy of the JAK inhibitor tofacitinib citrate in patients with alopecia areata

Milène Kennedy Crispin,1 Justin M. Ko,1 Brittany G. Craiglow,2,3 Shufeng Li,1 Gautam Shankar,1 Jennifer R. Urban,4 James C. Chen,5,6 Jane E. Cerise,5 Ali Jabbari,5 Mårten C.G. Winge,1 M. Peter Marinkovich,1 Angela M. Christiano,5,7 Anthony E. Oro,1 and Brett A. King2

, JCI Insight. 2016 Sep 22; 1(15): e89776.

This was a 2-center, open-label, single-arm trial using the pan-JAK inhibitor, tofacitinib citrate, for AA with >50% scalp hair loss, alopecia totalis (AT), and alopecia universalis (AU). Tofacitinib (5 mg) was given twice daily for 3 months. Endpoints included regrowth of scalp hair, as assessed by the severity of alopecia tool (SALT), duration of hair growth after completion of therapy, and disease transcriptome.

Tofacitinib (Xeljanz): The First-in-Class JAK Inhibitor for the Treatment of Rheumatoid Arthritis

Robert W. Dugger, Mark E. Flanagan, Rajappa Vaidyanathan

Innovative Drug Synthesis, 16 November 2015

Tofacitinib operates by inhibiting the JAK pathways utilized by several cytokines implicated in the pathogenesis of the disease. The SAR associated with the tofacitinib discovery program has been reported on extensively. Key elements of this medicinal chemistry program include the application of high-throughput-screening (HTS) to identify a lead molecule (5); and the early use of high-speed analoging (HSA).

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