Latar

Tofacitinib citrate, ogé katelah CP-690550 citrate, nyaéta inhibitor potent janus kinase 3 (JAK3), tirosin kinase anu diwatesan sél hematopoétik aub dina transduksi sinyal anu ngatur survival limfosit, proliferasi, diferensiasi, sareng apoptosis. Inhibisina nyaéta JAK3 spésifik sareng selektivitas 1000 kali langkung seueur tibatan kinase kulawarga non-JAK sanés. Di sagigireun ngahambat JAKS (IC50 = 1 nM), tofacitinib citrate ogé ngahambat janus kinase 2 (JAK2) sareng janus kinase 1 (JAK1) kalayan potency 20- sareng 100 kali langkung saeutik. Sanajan kitu, dina ulikan panganyarna, affinities mengikat (Ki) of tofacitinib citrate arah JAK1, JAK2, sarta JAK3 dilaporkeun janten 1.6 nM, 21.7 nM, sarta 6.5 nM mungguh.

Rujukan

Lalitha Vijayakrishnan, R. Venkataramanan jeung Palak Gulati. Ngubaran peradangan ku janus kinase inhibitor CP-690,550. Tren dina Élmu Farmakologi 2011: 32 (1); 25-34

Citer produk

• 1. Panagi I, Jennings E, et al. Salmonella Effector SteE Ngarobah Mammalian Serine/Threonine Kinase GSK3 jadi Tirosin Kinase pikeun Langsung Polarisasi Makrofag. Sél Host Mikroba. 2020;27(1):41–53.e6. PMID: 31862381
• 2. McInnes IB, Byers NL, et al. "Bandingan baricitinib, upadacitinib, sarta tofacitinib dimédiasi régulasi sinyal sitokin dina subpopulasi leukosit manusa." Rematik Res Ther. 2019 Agustus 2;21(1):183. PMID: 31375130
• 3. Liu S, Verma M, et al. "Resistansi stéroid sél lymphoid leuleuy tipe airway 2 ti penderita asma parna: Peran thymic stromal lymphopoietin." J Alergi Clin Immunol. 2018 Jan;141(1):257-268.e6. PMID: 28433687
• 4. Zheng, Lufeng, dkk. "The 3' UTR tina pseudogene CYP4Z2P promotes angiogenesis tumor dina kanker payudara ku akting salaku ceRNA pikeun CYP4Z1." Panalungtikan sarta pengobatan kanker payudara (2015): 1-14. PMID: 25701119

Katerangan

Tofacitinib citrate mangrupa inhibitor JAK1/2/3 oral sadia kalawan IC50s masing-masing 1, 20, jeung 112 nM. Tofacitinib citrate gaduh kagiatan antibakteri, antifungal sareng antiviral.

Panyimpenan

4 ° C, ngajaga tina cahaya

* Dina pangleyur: -80°C, 6 bulan; -20°C, 1 bulan (ngajagi tina cahaya)

Struktur kimiawi

Patali Data Biologis

Patali Data Biologis

Patali Data Biologis

Patali Data Biologis

Patali Data Biologis