Ruxolitinib free base | CAS#941678-49-5 | JAK Inhibitor

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

MedKoo CAT#: 201512

CAS#: 941678-49-5 (free base)

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.

Chemical Structure

Ruxolitinib free base

CAS# 941678-49-5 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 201512
Name: Ruxolitinib free base
CAS#: 941678-49-5 (free base)
Chemical Formula: C17H18N6
Exact Mass: 306.16
Molecular Weight: 306.370
Elemental Analysis: C, 66.65; H, 5.92; N, 27.43

Price and Availability

Size	Price	Availability
10mg	USD 90	Ready to ship
200mg	USD 250	Ready to ship
500mg	USD 450	Ready to Ship
1g	USD 750	Ready to ship
2g	USD 1350	Ready to Ship
5g	USD 2950	Ready to Ship
10g	USD 5250	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Appearance: White to light yellow solid powder

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

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#X7P07R31
View CoA: current batch, Lot#T7K08C28

QC Data:

View QC data: current batch, Lot#X7P07R31
View QC data: current batch, Lot#T7K08C28

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	Ruxolitinib is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.
In vitro activity:	Ruxolitinib exhibited significant in vitro activity against Nalm-6 cells. It dose-dependently inhibited cell proliferation, induced cell cycle arrest at G0/G1 phase, and promoted apoptosis in MLL-r ALL cells. Ruxolitinib inactivated the JAK/STAT signaling pathway, contributing to its anti-proliferative and pro-apoptotic effects. Ruxolitinib is a promising therapeutic agent for MLL-r leukemia. Reference: Transl Pediatr. 2023 Jun 30;12(6):1088-1097. https://pubmed.ncbi.nlm.nih.gov/37427069/
In vivo activity:	Ruxolitinib was administered to a patient with Epstein-Barr virus (EBV)-associated hemophagocytic lymphohistiocytosis (HLH) characterized by EBV infection within CD8+ T cells. Ruxolitinib treatment led to the resolution of symptoms and improvement in HLH parameters, demonstrating its in vivo activity in controlling EBV-associated HLH, particularly in cases where rituximab and corticosteroids may be insufficient. Reference: lin Transl Immunology. 2023 Jul 25;12(7):e1459. https://pubmed.ncbi.nlm.nih.gov/37497193/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	5.0	16.30
	DMF	5.0	16.30
	Ethanol	13.0	42.40

Preparing Stock Solutions

The following data is based on the product molecular weight 306.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Chen L, Zhu MY, Wang GX, Lu LL, Lin L, Lei L, Wu T. Ruxolitinib ameliorated coxsackievirus B3-induced acute viral myocarditis by suppressing the JAK-STAT pathway. Int Immunopharmacol. 2023 Aug 25;124(Pt A):110797. doi: 10.1016/j.intimp.2023.110797. Epub ahead of print. PMID: 37634445. 2. Liao XY, Zhou DH, Fang JP, Qiu KY. Ruxolitinib inhibits the proliferation and induces the apoptosis of MLL-r ALL cells through inactivating JAK/STAT signaling pathway. Transl Pediatr. 2023 Jun 30;12(6):1088-1097. doi: 10.21037/tp-23-16. Epub 2023 Jun 14. PMID: 37427069; PMCID: PMC10326758. 3. Ali S, Choo S, Hosking L, Smith A, Hughes T. A case of T-cell-Epstein-Barr virus-haemophagocytic lymphohistiocytosis and sustained remission following ruxolitinib therapy. Clin Transl Immunology. 2023 Jul 25;12(7):e1459. doi: 10.1002/cti2.1459. PMID: 37497193; PMCID: PMC10368518. 4. Berenson JR, Kim C, Bujarski S, To J, Spektor TM, Martinez D, Turner C, Ghermezi M, Eades BM, Swift RA, Schwartz G, Eshaghian S, Moss RA, Lim S, Vescio R. A phase 1 study of ruxolitinib, steroids and lenalidomide for relapsed/refractory multiple myeloma patients. Hematol Oncol. 2022 Dec;40(5):906-913. doi: 10.1002/hon.3066. Epub 2022 Aug 14. PMID: 35946431.
In vitro protocol:	1. Chen L, Zhu MY, Wang GX, Lu LL, Lin L, Lei L, Wu T. Ruxolitinib ameliorated coxsackievirus B3-induced acute viral myocarditis by suppressing the JAK-STAT pathway. Int Immunopharmacol. 2023 Aug 25;124(Pt A):110797. doi: 10.1016/j.intimp.2023.110797. Epub ahead of print. PMID: 37634445. 2. Liao XY, Zhou DH, Fang JP, Qiu KY. Ruxolitinib inhibits the proliferation and induces the apoptosis of MLL-r ALL cells through inactivating JAK/STAT signaling pathway. Transl Pediatr. 2023 Jun 30;12(6):1088-1097. doi: 10.21037/tp-23-16. Epub 2023 Jun 14. PMID: 37427069; PMCID: PMC10326758.
In vivo protocol:	1. Ali S, Choo S, Hosking L, Smith A, Hughes T. A case of T-cell-Epstein-Barr virus-haemophagocytic lymphohistiocytosis and sustained remission following ruxolitinib therapy. Clin Transl Immunology. 2023 Jul 25;12(7):e1459. doi: 10.1002/cti2.1459. PMID: 37497193; PMCID: PMC10368518. 2. Berenson JR, Kim C, Bujarski S, To J, Spektor TM, Martinez D, Turner C, Ghermezi M, Eades BM, Swift RA, Schwartz G, Eshaghian S, Moss RA, Lim S, Vescio R. A phase 1 study of ruxolitinib, steroids and lenalidomide for relapsed/refractory multiple myeloma patients. Hematol Oncol. 2022 Dec;40(5):906-913. doi: 10.1002/hon.3066. Epub 2022 Aug 14. PMID: 35946431.

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: Boldrini V, Vannucchi AM, Guglielmelli P. A safety evaluation of ruxolitinib for the treatment of polycythemia vera. Expert Opin Drug Saf. 2023 Dec 29:1-7. doi: 10.1080/14740338.2023.2299391. Epub ahead of print. PMID: 38156903.

2: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Ruxolitinib. 2023 Dec 15. PMID: 29999923.

3: Adesola AA, Cozma MA, Chen YF, Srichawla BS, Găman MA. Risk of hepatitis B reactivation in patients with myeloproliferative neoplasms treated with ruxolitinib. World J Hepatol. 2023 Nov 27;15(11):1188-1195. doi: 10.4254/wjh.v15.i11.1188. PMID: 38075009; PMCID: PMC10698348.

4: Yunianto I, Currie M, Chitcholtan K, Sykes P. Potential drug repurposing of ruxolitinib to inhibit the JAK/STAT pathway for the treatment of patients with epithelial ovarian cancer. J Obstet Gynaecol Res. 2023 Nov;49(11):2563-2574. doi: 10.1111/jog.15761. Epub 2023 Aug 10. PMID: 37565583.

5: Tavoletti G, Avallone G, Conforti C, Roccuzzo G, Maronese CA, Mattioli MA, Quaglino P, Zalaudek I, Marzano AV, Ribero S, Alberti-Violetti S. Topical ruxolitinib: A new treatment for vitiligo. J Eur Acad Dermatol Venereol. 2023 Nov;37(11):2222-2230. doi: 10.1111/jdv.19162. Epub 2023 May 15. PMID: 37147856.

6: Yan WL, Zhao FY, Gu ME, Liu N, Guo XP, Xu XJ. Ruxolitinib Treatment of Steroid-Refractory Graft-versus-Host Disease in Children: A Case Series and Review of the Literature. Paediatr Drugs. 2023 Sep;25(5):577-584. doi: 10.1007/s40272-023-00577-8. Epub 2023 Jun 7. PMID: 37284944.

7: Al Sharie AH, Abu Mousa BM, Alomari AO. Incorporation of Ruxolitinib in the Management of Refractory/Relapsed Hodgkin Lymphoma: Where Do We Stand? Clin Hematol Int. 2023 Aug 28;5(4):1-4. doi: 10.46989/001c.87501. PMID: 37752987; PMCID: PMC10515879.

8: Hwang JR, Driscoll MS. Review of Ruxolitinib for Treatment of Non-Segmental Vitiligo. Ann Pharmacother. 2023 Aug;57(8):948-955. doi: 10.1177/10600280221143748. Epub 2022 Dec 23. PMID: 36564903.

9: Verstovsek S, Mesa RA, Livingston RA, Hu W, Mascarenhas J. Ten years of treatment with ruxolitinib for myelofibrosis: a review of safety. J Hematol Oncol. 2023 Jul 27;16(1):82. doi: 10.1186/s13045-023-01471-z. PMID: 37501130; PMCID: PMC10373260.

10: Algeri M, Becilli M, Locatelli F. Ruxolitinib as the first post-steroid treatment for acute and chronic graft-versus-host disease. Expert Rev Clin Immunol. 2023 Jul-Dec;19(11):1299-1313. doi: 10.1080/1744666X.2023.2249230. Epub 2023 Aug 22. PMID: 37606511.

11: Pemmaraju N, Bose P, Rampal R, Gerds AT, Fleischman A, Verstovsek S. Ten years after ruxolitinib approval for myelofibrosis: a review of clinical efficacy. Leuk Lymphoma. 2023 Jun;64(6):1063-1081. doi: 10.1080/10428194.2023.2196593. Epub 2023 Apr 20. PMID: 37081809.

12: Mancuso-Stewart E, DiRuggiero M, DiRuggiero D, Zirwas M. New Non-Steroidal Topical Therapies for Inflammatory Dermatoses-Part 1: Ruxolitinib. Skinmed. 2023 May 9;21(2):93-98. PMID: 37158346.

13: Kashetsky N, Turchin I. Utilization of Topical Ruxolitinib in Dermatology: A Review. Skin Therapy Lett. 2023 May;28(3):8-13. PMID: 37339609.

14: Krajewski PK, Szepietowski JC. Ruxolitinib cream for the short-term treatment of mild-moderate atopic dermatitis. Expert Rev Clin Immunol. 2023 Apr;19(4):349-356. doi: 10.1080/1744666X.2023.2161511. Epub 2022 Dec 26. PMID: 36542765.

15: Mohney LA, Singh R, Feldman SR. Review of Ruxolitinib in the Treatment of Atopic Dermatitis. Ann Pharmacother. 2023 Feb;57(2):207-216. doi: 10.1177/10600280221103282. Epub 2022 Jun 8. PMID: 35674400.

16: Hoy SM. Ruxolitinib Cream 1.5%: A Review in Mild to Moderate Atopic Dermatitis. Am J Clin Dermatol. 2023 Jan;24(1):143-151. doi: 10.1007/s40257-022-00748-2. Epub 2022 Dec 20. Erratum in: Am J Clin Dermatol. 2023 May;24(3):495. PMID: 36538235; PMCID: PMC10036407.

17: Li GM, Jin YB, Gan YZ, Chen C, Jia Y, Li C. [Ruxolitinib as an effective treatment for panniculitis associated hemophagocytic syndrome: A report of 2 cases and literature review]. Beijing Da Xue Xue Bao Yi Xue Ban. 2022 Dec 18;54(6):1208-1213. Chinese. doi: 10.19723/j.issn.1671-167X.2022.06.025. PMID: 36533357; PMCID: PMC9761834.

18: Devos T, Selleslag D, Granacher N, Havelange V, Benghiat FS. Updated recommendations on the use of ruxolitinib for the treatment of myelofibrosis. Hematology. 2022 Dec;27(1):23-31. doi: 10.1080/16078454.2021.2009645. PMID: 34957926.

19: Sadeghi S, Goodarzi A. Various Application of Tofacitinib and Ruxolitinib (Janus Kinase Inhibitors) in Dermatology and Rheumatology: A Review of Current Evidence and Future Perspective. Dermatol Pract Concept. 2022 Oct 1;12(4):e2022178. doi: 10.5826/dpc.1204a178. PMID: 36534552; PMCID: PMC9681403.

20: Owji S, Caldas SA, Ungar B. Management of Atopic Dermatitis: Clinical Utility of Ruxolitinib. J Asthma Allergy. 2022 Oct 25;15:1527-1537. doi: 10.2147/JAA.S342051. PMID: 36316998; PMCID: PMC9617518.

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