Ruxolitinib free base

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Ruxolitinib, also known as INC424 and INCB18424 or INCB018424,is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.

Price and Availability

Ruxolitinib free base, purity > 98%, is in stock. The same day shipping out after order received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 201512Name: Ruxolitinib free baseCAS#: 941678-49-5 (free base)Chemical Formula: C17H18N6Exact Mass: 306.15929Molecular Weight: 306.37Elemental Analysis:C, 66.65; H, 5.92; N, 27.43

Related CAS #:941678-49-5 (free base)1092939-17-7 (phosphate)

Synonym:INCB018424; INCB 018424; INCB-018424; INC424; INC424; INC-424; INCB18424; INCB 18424; INCB-18424; trade name:J akafi and Jakavi

IUPAC/Chemical Name:(R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

InChi Key:HFNKQEVNSGCOJV-OAHLLOKOSA-N

InChi Code: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

SMILES Code:N#CC[C@@H](N1N=CC(C2=C3C(NC=C3)=NC=N2)=C1)C4CCCC4

Technical Data

References

1: Santos FP, Verstovsek S. Efficacy of ruxolitinib for myelofibrosis. Expert Opin Pharmacother. 2014 Jul;15(10):1465-73. doi: 10.1517/14656566.2014.923404. Epub 2014 May 24. Review. PubMed PMID: 24856675.

2: Molica M, Serrao A, Saracino R, Zacheo I, Stingone C, Alimena G, Breccia M. Disappearance of fibrosis in secondary myelofibrosis after ruxolitinib treatment: new endpoint to achieve? Ann Hematol. 2014 Nov;93(11):1951-2. doi: 10.1007/s00277-014-2096-y. Epub 2014 May 7. Review. PubMed PMID: 24801017.

3: Becker H, Engelhardt M, von Bubnoff N, Wäsch R. Ruxolitinib. Recent Results Cancer Res. 2014;201:249-57. doi: 10.1007/978-3-642-54490-3_16. Review. PubMed PMID: 24756798.

4: Swaim SJ. Ruxolitinib for the treatment of primary myelofibrosis. Am J Health Syst Pharm. 2014 Mar 15;71(6):453-62. doi: 10.2146/ajhp120602. Review. PubMed PMID: 24589536.

5: Mesa RA, Cortes J. Optimizing management of ruxolitinib in patients with myelofibrosis: the need for individualized dosing. J Hematol Oncol. 2013 Oct 22;6:79. doi: 10.1186/1756-8722-6-79. Review. PubMed PMID: 24283870; PubMed Central PMCID: PMC4222119.

6: Kantarjian HM, Silver RT, Komrokji RS, Mesa RA, Tacke R, Harrison CN. Ruxolitinib for myelofibrosis--an update of its clinical effects. Clin Lymphoma Myeloma Leuk. 2013 Dec;13(6):638-45. doi: 10.1016/j.clml.2013.09.006. Epub 2013 Oct 2. Review. PubMed PMID: 24238036.

7: Harrison C, Mesa R, Ross D, Mead A, Keohane C, Gotlib J, Verstovsek S. Practical management of patients with myelofibrosis receiving ruxolitinib. Expert Rev Hematol. 2013 Oct;6(5):511-23. doi: 10.1586/17474086.2013.827413. Epub 2013 Oct 2. Review. PubMed PMID: 24083419.

8: Wade R, Rose M, Neilson AR, Stirk L, Rodriguez-Lopez R, Bowen D, Craig D, Woolacott N. Ruxolitinib for the treatment of myelofibrosis: a NICE single technology appraisal. Pharmacoeconomics. 2013 Oct;31(10):841-52. doi: 10.1007/s40273-013-0083-0. Review. PubMed PMID: 23996108.

9: Lemal R, Robin M, Ravinet A, Cacheux V, Guièze R, Bay JO. [Ruxolitinib prescription in myelofibrosis]. Bull Cancer. 2013 Sep;100(9):897-902. doi: 10.1684/bdc.2013.1792. Review. French. PubMed PMID: 23985569.

10: Kremyanskaya M, Atallah EL, Hoffman R, Mascarenhas JO. Clarifying the use of ruxolitinib in patients with myelofibrosis. Oncology (Williston Park). 2013 Jul;27(7):706-14. Review. Erratum in: Oncology (Williston Park). 2013 Aug;27(8):737. PubMed PMID: 23977767.

11: Mascarenhas J, Hoffman R. A comprehensive review and analysis of the effect of ruxolitinib therapy on the survival of patients with myelofibrosis. Blood. 2013 Jun 13;121(24):4832-7. doi: 10.1182/blood-2013-02-482232. Epub 2013 Apr 9. Review. PubMed PMID: 23570800.

12: Verstovsek S. Ruxolitinib: an oral Janus kinase 1 and Janus kinase 2 inhibitor in the management of myelofibrosis. Postgrad Med. 2013 Jan;125(1):128-35. doi: 10.3810/pgm.2013.01.2628. Review. PubMed PMID: 23391678.

13: Ganetsky A. Ruxolitinib: a new treatment option for myelofibrosis. Pharmacotherapy. 2013 Jan;33(1):84-92. doi: 10.1002/phar.1165. Review. PubMed PMID: 23307549.

14: Vaddi K, Sarlis NJ, Gupta V. Ruxolitinib, an oral JAK1 and JAK2 inhibitor, in myelofibrosis. Expert Opin Pharmacother. 2012 Nov;13(16):2397-407. doi: 10.1517/14656566.2012.732998. Epub 2012 Oct 10. Review. PubMed PMID: 23051187.

15: Mascarenhas J, Mughal TI, Verstovsek S. Biology and clinical management of myeloproliferative neoplasms and development of the JAK inhibitor ruxolitinib. Curr Med Chem. 2012;19(26):4399-413. Review. PubMed PMID: 22830345; PubMed Central PMCID: PMC3480698.

16: Ruxolitinib (Jakafi) for myelofibrosis. Med Lett Drugs Ther. 2012 Apr 2;54(1387):27-8. Review. PubMed PMID: 22469651.

17: Ostojic A, Vrhovac R, Verstovsek S. Ruxolitinib for the treatment of myelofibrosis. Drugs Today (Barc). 2011 Nov;47(11):817-27. doi: 10.1358/dot.2011.47.11.1708829. Review. PubMed PMID: 22146225.

18: Naqvi K, Verstovsek S, Kantarjian H, Ravandi F. A potential role of ruxolitinib in leukemia. Expert Opin Investig Drugs. 2011 Aug;20(8):1159-66. doi: 10.1517/13543784.2011.589383. Epub 2011 Jun 3. Review. PubMed PMID: 21635221; PubMed Central PMCID: PMC4143907.