Keeb kwm

Tofacitinib citrate, tseem hu ua CP-690550 citrate, yog ib qho muaj zog inhibitor ntawm janus kinase 3 (JAK3), hematopoetic cell-txheej txheem tyrosine kinase koom nrog hauv cov teeb liab transduction tswj lymphocyte ciaj sia, proliferation, sib txawv, thiab apoptosis. Qhov inhibition yog JAK3 tshwj xeeb nrog kev xaiv 1000-fold ntau dua li lwm yam tsis yog JAK tsev neeg kinases. Dhau li ntawm inhibiting JAKS (IC50 = 1 nM), tofacitinib citrate kuj inhibits janus kinase 2 (JAK2) thiab janus kinase 1 (JAK1) nrog 20- thiab 100-fold tsawg dua hauv potency feem. Txawm li cas los xij, hauv kev tshawb fawb tsis ntev los no, kev sib koom ua ke (Ki) ntawm tofacitinib citrate rau JAK1, JAK2, thiab JAK3 tau tshaj tawm tias yog 1.6 nM, 21.7 nM, thiab 6.5 nM feem.

Kev siv

Lalitha Vijayakrishnan, R. Venkataramanan thiab Palak Gulati. Kev kho mob nrog rau janus kinase inhibitor CP-690,550. Trends in Pharmacological Sciences 2011: 32 (1); 25-34 : kuv

Khoom Citation

• 1. Panagi I, Jennings E, et al. "Salmonella Effector SteE Hloov Cov Mammalian Serine / Threonine Kinase GSK3 rau hauv Tyrosine Kinase rau Direct Macrophage Polarization." Cell Host Microbe. 2020; 27(1):41–53.e6. PIB: 31862381
• 2. McInnes IB, Byers NL, et al. "Kev sib piv ntawm baricitinib, upadacitinib, thiab tofacitinib kho cov kev cai ntawm cytokine signaling nyob rau hauv tib neeg leukocyte subpopulations." Arthritis Res Ther. Peb Hlis 21, 2019: 183. PIB: 31375130
• 3. Liu S, Verma M, et al. "Steroid resistance of airway type 2 innate lymphoid cells los ntawm cov neeg mob uas muaj mob hawb pob: Lub luag haujlwm ntawm thymic stromal lymphopoietin." J Allergy Clin Immunol. 2018 Jan;141(1):257-268.e6. PIB: 28433687
• 4. Zheng, Xu, et al. "Lub 3′ UTR ntawm pseudogene CYP4Z2P txhawb qog angiogenesis hauv qog noj ntshav los ntawm kev ua raws li ceRNA rau CYP4Z1." Kev tshawb fawb thiab kev kho mob cancer mis (2015): 1-14. PIB: 25701119

Kev piav qhia

Tofacitinib citrate yog qhov ncauj muaj JAK1/2/3 inhibitor nrog IC50s ntawm 1, 20, thiab 112 nM, raws li. Tofacitinib citrate muaj cov tshuaj tua kab mob, tshuaj tua kab mob thiab tshuaj tua kab mob.

Cia

4 ° C, tiv thaiv lub teeb

* Nyob rau hauv hnyav: -80 ° C, 6 lub hlis; -20 ° C, 1 lub hlis (tiv thaiv lub teeb)

Cov qauv tshuaj

Cov ntaub ntawv ntsig txog Biological

Cov ntaub ntawv ntsig txog Biological

Cov ntaub ntawv ntsig txog Biological

Cov ntaub ntawv ntsig txog Biological

Cov ntaub ntawv ntsig txog Biological