Fedratinib - CAS 936091-26-8
Catalog number: B0084-100796
Category: Inhibitor
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Fedratinib is a potent and selective JAK2 inhibitor with IC50 value of 6 nM. It also exhibits inhibitory effects against FLT3 (IC50 = 25 nM), RET (IC50 = 17 nM) and JAK3 (IC50 = 169 nM).
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B0084-100796 25 mg $198 In stock
B0084-100796 50 mg $298 In stock
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TG101348; SAR302503; N-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
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1.Decrease of Store-Operated Ca2+ Entry and Increase of Na+/Ca2+ Exchange by Pharmacological JAK2 Inhibition.
Yan J1, Hosseinzadeh Z, Zhang B, Froeschl M, Schulze-Osthoff K, Stournaras C, Lang F. Cell Physiol Biochem. 2016;38(2):683-95. doi: 10.1159/000443126. Epub 2016 Feb 8.
BACKGROUND/AIMS: Cell proliferation and migration are regulated by cytosolic Ca2+ activity ([Ca2+]i). Mechanisms modifying [Ca2+]i include store-operated Ca2+-entry (SOCE) accomplished by the pore-forming ion channel unit Orai1 and its regulator STIM1, as well as Ca2+ extrusion by Na+/Ca2+ exchanger NCX1. Kinases participating in the orchestration of cell proliferation include the Janus activated kinase JAK2. The present study explored the impact of pharmacological JAK2 inhibition on SOCE and Na+/Ca2+ exchange.
2.Safety and Efficacy of Fedratinib in Patients With Primary or Secondary Myelofibrosis: A Randomized Clinical Trial.
Pardanani A1, Harrison C2, Cortes JE3, Cervantes F4, Mesa RA5, Milligan D6, Masszi T7, Mishchenko E8, Jourdan E9, Vannucchi AM10, Drummond MW11, Jurgutis M12, Kuliczkowski K13, Gheorghita E14, Passamonti F15, Neumann F16, Patki A16, Gao G16, Tefferi A1. JAMA Oncol. 2015 Aug;1(5):643-51. doi: 10.1001/jamaoncol.2015.1590.
IMPORTANCE: Myelofibrosis (MF) is a BCR-ABL-negative myeloproliferative neoplasm characterized by anemia, splenomegaly, debilitating constitutional symptoms, and shortened survival. Fedratinib, a JAK2-selective inhibitor, previously demonstrated clinically beneficial activity in patients with MF in early-phase trials.
3.JAK inhibition induces silencing of T Helper cytokine secretion and a profound reduction in T regulatory cells.
Keohane C1,2, Kordasti S2,3, Seidl T2, Perez Abellan P2, Thomas NS2, Harrison CN1, McLornan DP1,3, Mufti GJ2,3. Br J Haematol. 2015 Oct;171(1):60-73. doi: 10.1111/bjh.13519. Epub 2015 Jun 15.
CD4(+) T cells maintain cancer surveillance and immune tolerance. Chronic inflammation has been proposed as a driver of clonal evolution in myeloproliferative neoplasms (MPN), suggesting that T cells play an important role in their pathogenesis. Treatment with JAK inhibitors (JAKi) results in improvements in MPN-associated constitutional symptoms as well as reductions in splenomegaly. However, effects of JAKi on T cells in MPN are not well established and the baseline immune signature remains unclear. We investigated the frequency and function of CD4(+) T cell subsets in 50 MPN patients at baseline as well as during treatment with either ruxolitinib or fedratinib in a subset. We show that CD4(+)  CD127(low)  CD25(high)  FOXP3(+) T regulatory cells are reduced in MPN patients compared to healthy controls and that this decrease is even more pronounced following JAKi therapy. Moreover, we show that after 6 months of treatment the number of T helper (Th)-17 cells increased.
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CAS 936091-26-8 Fedratinib

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