CAS 941678-49-5 Ruxolitinib wird bei der Behandlung von Myeloproliferativen Neoplasmen und Psoriasis verwendet.

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CAS 941678-49-5 Ruxolitinib Used in The Treatment of Myeloproliferative Neoplasms and Psoriasis.
CAS 941678-49-5 Ruxolitinib Used in The Treatment of Myeloproliferative Neoplasms and Psoriasis.
Description In November 2011, the U.S. FDA approved ruxolitinib (INCB018424) for the treatment of patients with intermediate or high-risk myelofibrosis. Ruxolitinib is an ATP-competitive inhibitor of JAK1 and JAK2 (IC 50's  of 3.3±1.2 nM and 2.8±1.2 nM, respectively) and inhibition occurs regardless of the JAK2V617F mutational status. Ruxolitinib is a moderately potent inhibitor of the related JAK, TYK2 (IC 50 =19±3.2 nM) but is selective versus JAK3 (IC 50 =428±243 nM). It was also selective versus a panel of 26 other kinases at concentrations approximately 100-fold the IC 50  of JAK1 and JAK2. Inhibition of JAK1 and JAK2 downregulates the JAK-signal transducer and activator of transcription (STAT) pathway, inhibiting myeloproliferation, inducing apoptosis, and reducing numerous cytokine plasma levels.
Originator Incyte Corporation (United States)
Uses Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines. A JAK2 gene fusion mutation, JAK2V617F, that causes unchecked activation of various and cytokines, has been linked to myeloproliferative neoplasms (MPNs), including polycythemia vera, essential thrombocythemia, and primary myelofibrosis. Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC50 = 322 nM). It can block interleukin-6 (IL-6) signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM). In primary cultures, ruxolitinib preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ polycythemia vera patients (IC50 = 67 nM) versus healthy donors (IC50 > 400 nM). In a mouse model of JAK2V617F+ MPN, 90 mg/kg ruxolitinib reduced splenomegaly, decreased circulating levels of IL-6 and TNF-α, eliminated neoplastic cells, and prolonged survival of the treated animals.[Cayman Chemical]
Uses A JAK family kinase inhibitor of JAK1, JAK2 and JAK3 with IC50s of 2.7 nM, 4.5 nM and 322 nM, respectively
Uses Ruxolitinib is a selective Janus tyrosine kinase (JAK1 and JAK2) inhibitor used in the treatment of myeloproliferative neoplasms and psoriasis.
Uses INCB018424 is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3
Definition ChEBI: A pyrazole substituted at position 1 by a 2-cyano-1-cyclopentylethyl group and at position 3 by a pyrrolo[2,3-d]pyrimidin-4-yl group. Used as the phosphate salt for the treatment of patients with intermediate or high-risk myelofibrosis, includ ng primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis.
Indications The JAK family includes four isoforms, JAK1, JAK2, JAK3, and tyrosine kinase (TYK2). Ruxolitinib (Jakafi(R), Incyte Corp.) was the first approved JAK inhibitor, which inhibits both JAK1 and JAK2, used for the treatment of different types of myelofibrosis. Tofacitinib (Xeljanz(R), Pfizer) was approved by FDA as a JAK3-selective inhibitor for the treatment of rheumatoid arthritis and is one of the only two FDA-approved kinase inhibitors for non-oncological indications.
Clinical Use Tyrosine kinase inhibitor:
Treatment of disease related splenomegaly or symptoms in patients with primary myelofibrosis (MF), post polycythaemia vera (PV) myelofibrosis or post-essential thrombocythemia myelofibrosis
Drug interactions Potentially hazardous interactions with other drugs
Antibacterials: concentration increased by clarithromycin and telithromycin, reduced dose of ruxolitinib; concentration reduced by rifampicin.
Antifungals: reduce dose of ruxolitinib with fluconazole, itraconazole, ketoconazole, posaconazole and voriconazole.
Antipsychotics: avoid with clozapine, risk of agranulocytosis.
Antivirals: reduce dose of ruxolitinib with boceprevir, indinavir, lopinavir, ritonavir, saquinavir and telaprevir.
CAS 941678-49-5 Ruxolitinib Used in The Treatment of Myeloproliferative Neoplasms and Psoriasis.
CAS 941678-49-5 Ruxolitinib Used in The Treatment of Myeloproliferative Neoplasms and Psoriasis.
Hubei weideli Chemical Reagent Co., Ltd., located in Wuhan East Lake New Technology Development Zone, is a manufacturing supplier focusing on reagent products for scientific research, and its business scope includes the manufacturing of special chemical products; Disinfectant production; Sales of special chemical products; Disinfectant sales; Research and development of biological feed; Research and development of bio based materials technology; Research and development of biochemical products technology; Technical services, technical development, technical consultation, technical exchange, technology transfer and technology promotion; Sales of instruments and meters; Sales of daily glass products; Sales of technical glass products; Sales of electronic special materials; Technology import and export; Import and export of goods; Veterinary drug management; Production of disinfection products for the prevention and treatment of infectious diseases.

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