Ruxolitinib - CAS 941678-49-5
Catalog number: B0084-156872
Category: Inhibitor
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Molecular Formula:
C17H18N6
Molecular Weight:
306.37
COA:
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Targets:
JAK
Description:
Ruxolitinib is a potent and selective JAK1/2 inhibitor with IC50 values of 3.3 nM and 2.8 nM respectively in cell-free assays, and has > 130-fold selectivity for JAK1/2 versus JAK3.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-156872 200 mg $198 In stock
B0084-156872 500 mg $398 In stock
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Appearance:
White to Off-white Solid
Synonyms:
(R)-Ruxolitinib; INCB018424; R-INCB018424; (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile
MSDS:
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Melting Point:
84-89°C
InChIKey:
HFNKQEVNSGCOJV-OAHLLOKOSA-N
InChI:
InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1
Canonical SMILES:
C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
1.Captopril mitigates splenomegaly and myelofibrosis in the Gata1
Corey SJ;Jha J;McCart EA;Rittase WB;George J;Mattapallil JJ;Mehta H;Ognoon M;Bylicky MA;Summers TA;Day RM J Cell Mol Med. 2018 Sep;22(9):4274-4282. doi: 10.1111/jcmm.13710. Epub 2018 Jul 4.
Allogeneic stem cell transplantation is currently the only curative therapy for primary myelofibrosis (MF), while the JAK2 inhibitor, ruxolitinib. Has been approved only for palliation. Other therapies are desperately needed to reverse life-threatening MF. However, the cell(s) and cytokine(s) that promote MF remain unclear. Several reports have demonstrated that captopril, an inhibitor of angiotensin-converting enzyme that blocks the production of angiotensin II (Ang II), mitigates fibrosis in heart, lung, skin and kidney. Here, we show that captopril can mitigate the development of MF in the Gata1;low; mouse model of primary MF. Gata1;low; mice were treated with 79 mg/kg/d captopril in the drinking water from 10 to 12 months of age. At 13 months of age, bone marrows were examined for fibrosis, megakaryocytosis and collagen expression; spleens were examined for megakaryocytosis, splenomegaly and collagen expression. Treatment of Gata1;low; mice with captopril in the drinking water was associated with normalization of the bone marrow cellularity; reduced reticulin fibres, splenomegaly and megakaryocytosis; and decreased collagen expression. Our findings suggest that treating with the ACE inhibitors captopril has a significant benefit in overcoming pathological changes associated with MF.
2.Practical Measures of Clinical Benefit With Ruxolitinib Therapy: An Exploratory Analysis of COMFORT-I.
Miller CB;Komrokji RS;Mesa RA;Sun W;Montgomery M;Verstovsek S Clin Lymphoma Myeloma Leuk. 2017 Aug;17(8):479-487. doi: 10.1016/j.clml.2017.05.015. Epub 2017 May 12.
BACKGROUND: ;The phase III COMFORT (Controlled Myelofibrosis Study With Oral JAK inhibitor Treatment)-I and COMFORT-II trials in patients with intermediate-2 or high-risk myelofibrosis (MF) showed that ruxolitinib was superior to placebo and best available therapy, respectively, for improvements in spleen volume, MF-related symptoms, and overall survival (OS). However, patients managed in community settings might not have access to the methods used in the COMFORT trials. In this exploratory analysis we summarize efficacy findings of COMFORT-I using practical, community-oriented measures of patient outcomes.;PATIENTS AND METHODS: ;In this post hoc analysis of data from COMFORT-I we evaluated changes from baseline to week 12 in spleen size (palpable length and volume), patient-reported outcomes (Patient Global Impression of Change; Myelofibrosis Symptom Assessment Form; Patient-Reported Outcomes Measurement System Fatigue Scale), body weight, and serum albumin levels in 5 subgroups of ruxolitinib-treated patients on the basis of week 12 spleen length changes from baseline: (1-4) ≥ 50%, 25% to < 50%, 10% to < 25%, or < 10% reduction; and (5) worsening. OS was evaluated in ruxolitinib-treated patients with week 12 spleen length reductions from baseline ≥ 50%, 25% to < 50%, or < 25% (including worsening).
3.Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.
Kettle JG;Åstrand A;Catley M;Grimster NP;Nilsson M;Su Q;Woessner R Expert Opin Ther Pat. 2017 Feb;27(2):145-161. doi: 10.1080/13543776.2017.1252754. Epub 2016 Nov 4.
Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly linked to both cancer and inflammatory diseases. There are currently two launched JAK inhibitors for the treatment of human conditions: tofacitinib for Rheumatoid arthritis (RA) and ruxolitinib for myeloproliferative neoplasms including intermediate or high risk myelofibrosis and polycythemia vera. Areas covered: This review covers patents claiming activity against one or more JAK family members in the period 2013-2015 inclusive, and covers 95 patents from 42 applicants, split over two parts. The authors have ordered recent patents according to the primary applicant's name, with part 2 covering J through Z. Expert opinion: Inhibition of JAK-family kinases is an area of growing interest, catalysed by the maturity of data on marketed inhibitors ruxolitinib and tofacitinib in late stage clinical trials. Many applicants are pursuing traditional fast-follower strategies around these inhibitors, with a range of chemical strategies adopted. The challenge will be to show sufficient differentiation to the originator compounds, since dose limiting toxicities with such agents appear to be on target and mechanism-related and also considering that such agents may be available as generic compounds by the time follower agents reach market.
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CAS 941678-49-5 Ruxolitinib

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