WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H201512
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.
Hodoodo Cat#: H201512
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
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
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.0 | 16.30 | |
| DMF | 5.0 | 16.30 | |
| Ethanol | 13.0 | 42.40 |
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: | |
| In vitro protocol: | |
| In vivo protocol: |
: 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.
