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Best-Selling Boceprevir And Telaprevir - Tofacitnib Citrate – CPF

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  • Best-Selling Boceprevir And Telaprevir - Tofacitnib Citrate – CPF

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Best-Selling Boceprevir And Telaprevir - Tofacitnib Citrate – CPF Detail:

Background

Tofacitinib citrate, also known as CP-690550 citrate, is a potent inhibitor of janus kinase 3 (JAK3), a hematopoetic cell-restricted tyrosine kinase involved in signal transduction regulating lymphocyte survival, proliferation, differentiation, and apoptosis.  The inhibition is JAK3 specific with a selectivity 1000-fold more than other non-JAK family kinases. Besides inhibiting JAKS (IC50 = 1 nM), tofacitinib citrate also inhibits janus kinase 2 (JAK2) and janus kinase 1 (JAK1) with 20- and 100-fold less in potency respectively. However, in a recent study, the binding affinities (Ki) of tofacitinib citrate towards JAK1, JAK2, and JAK3 were reported to be 1.6 nM, 21.7 nM, and 6.5 nM respectively.

Reference

Lalitha Vijayakrishnan, R. Venkataramanan and Palak Gulati. Treating inflammation with the janus kinase inhibitor CP-690,550. Trends in Pharmacological Sciences 2011: 32 (1); 25-34

Product Citation

  • 1. Panagi I, Jennings E, et al. “Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization.” Cell Host Microbe. 2020;27(1):41–53.e6. PMID:31862381
  • 2. McInnes IB, Byers NL, et al. “Comparison of baricitinib, upadacitinib, and tofacitinib mediated regulation of cytokine signaling in human leukocyte subpopulations.” Arthritis Res Ther. 2019 Aug 2;21(1):183. PMID:31375130
  • 3. Liu S, Verma M, et al. “Steroid resistance of airway type 2 innate lymphoid cells from patients with severe asthma: The role of thymic stromal lymphopoietin.”J Allergy Clin Immunol. 2018 Jan;141(1):257-268.e6. PMID:28433687
  • 4. Zheng, Lufeng, et al. “The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1.” Breast cancer research and treatment (2015): 1-14. PMID:25701119

Description

Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

 

Chemical structure

Tofacitnib Citrate

Related Biological Data

Tofacitnib Citrate2

Related Biological Data

Tofacitnib Citrate3

Related Biological Data

Tofacitnib Citrate4

Related Biological Data

Tofacitnib Citrate5

Related Biological Data

Tofacitnib Citrate6

2018 GMP-2
原料药GMP证书201811（captopril ,thalidomide etc）
GMP-of-PMDA-in-Chanyoo-平成28年08月03日　Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

OUR STRENGTH

Quality management1

Proposal 18 Quality Consistency Evaluation projects which have approved 4, and 6 projects are under approving.

Quality management2

Advanced international quality management system has laid solid foundation for sales.

Quality management3

Quality supervision runs through the whole life cycle of the product to ensure the quality and therapeutic effect. 

Quality management4

Professional Regulatory Affairs team supports the quality demands during the application and registration.


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