Ruxolitinib . phosphate salt
AG-CR1-3645-M0055 mgCHF 50.00
AG-CR1-3645-M02525 mgCHF 120.00
|Synonyms||INCB018424; INC 424|
|Formula||C17H18N6 . H3O4P|
|MW||306.4 . 98.0|
|Purity Chemicals||≥98% (HPLC)|
|Appearance||White to off-white solid.|
|Solubility||Soluble in DMSO (>100mg/ml) and water (8mg/ml). Slightly soluble in 100% ethanol.|
|Identity||Determined by 1H-NMR and MS.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Handling Advice||Keep cool and dry.|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Water-soluble phosphate salt of Ruxolitinib.
- Antineoplastic, anti-inflammatory and immunomodulating agent.
- Orally bioavailable potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5nM, respectively and is less selective for JAK3 (IC50=322nM).
- Affects DC differentiation and function, leading to impaired T cell activation.
- Used in the treatment of myeloproliferative neoplasms and psoriasis.
- Anticancer agent. Shown to induce apoptosis and autophagy.
- Potent and selective inhibitor of HIV-1 replication and virus reactivation in vitro.
- Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction: Q. Lin, et al.; Org. Lett. 11, 1999 (2009)
- Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms: A. Quintas-Cardama, et al.; Blood 115, 3109 (2010)
- Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050: J.S. Fridman, et al.; J. Immunol. 184, 5298 (2010)
- Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis: R.A. Mesa; IDrugs 13, 394 (2010)
- The JAK-inhibitor ruxolitinib impairs dendritic cell function in vitro and in vivo: A. Heine, et al.; Blood 122, 1192 (2013)
- Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348): T. Zhou, et al.; Leukemia 28, 404 (2014)
- Tumoricidal effects of the JAK inhibitor Ruxolitinib (INC424) on hepatocellular carcinoma in vitro: G.S. Wilson, et al.; Cancer Lett. 341, 224 (2013)
- INCB018424 induces apoptotic cell death through the suppression of pJAK1 in human colon cancer cells: H.J. An, et al.; Neoplasma 61, 56 (2014)
- Ruxolitinib is a potent immunosuppressive compound: is it time for anti-infective prophylaxis? A. Heine, et al.; Blood 122, 3843 (2013)
- Ruxolitinib and tofacitinib are potent and selective inhibitors of HIV-1 replication and virus reactivation in vitro: C. Gavegnano, et al.; Antimicrob. Agents Chemother. 58, 1977 (2014)
- Ruxolitinib induces autophagy in chronic myeloid leukemia cells: B.G. Bagca, et al.; Tumour Biol. 37, 1573 (2016)