Ruxolitinib phosphate
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MedKoo CAT#: 120209

CAS#: 1092939-17-7 (phosphate)

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

Size
Price

50mg
USD 90
500mg
USD 450
5g
USD 2850
Size
Price

100mg
USD 150
1g
USD 650
10g
USD 4650
Size
Price

200mg
USD 250
2g
USD 1250
20g
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Ruxolitinib phosphate, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 20g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 120209
Name: Ruxolitinib phosphate
CAS#: 1092939-17-7 (phosphate)
Chemical Formula: C17H21N6O4P
Exact Mass: 404.13619
Molecular Weight: 404.37
Elemental Analysis:


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

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

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

InChi Key: JFMWPOCYMYGEDM-XFULWGLBSA-N

InChi Code: InChI=1S/C17H18N6.H3O4P/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;1-5(2,3)4/h6,8-12,15H,1-5H2,(H,19,20,21);(H3,1,2,3,4)/t15-;/m1./s1

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


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Ruxolitinib is a drug being investigated for the treatment of myeloproliferative diseases, plaque psoriasis, and various types of cancer. It is a Janus kinase inhibitor with selectivity for subtypes 1 and 2 of this enzyme.  Roxolitinib is being marketed by Incyte Pharmaceuticals and Novartis under the trade name Jakafi. Results from Phase II clinical trials suggest that the drug can substantially improve symptoms and reduce spleen size in myelofibrosis patients, but it has not been shown to produce remission.[4] As of February 2011, it is undergoing Phase III trials studying myelofibrosis  and polycythemia vera. In June 2011, it was announced that both phase III trials of ruxolitinib in the treatment of myelofibrosis (COMFORT-I and -II) met their primary endpoints of a significant increase in number of patients experiencing at least 35% reduction of spleen volume. In November 2011, Ruxolitinib was approved by the U.S. Food and Drug Administration for the treatment of intermediate or high-risk myelofibrosis based on results of the COMFORT-I and COMFORT-II Trials. (source: http://en.wikipedia.org/wiki/Ruxolitinib).
 
 


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.