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Ruxolitinib . phosphate salt

AG-CR1-3645-M005 5 mg INQ
AG-CR1-3645-M025 25 mg INQ
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Additional Information

Product Data
Synonyms INCB018424; INC 424
Properties
Formula C17H18N6 . H3O4P
MW 306.4 . 98.0
CAS 1092939-17-7
Purity ≥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.
InChi Key JFMWPOCYMYGEDM-XFULWGLBSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
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.
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Product Description

  • 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.

Product References

  1. Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction: Q. Lin, et al.; Org. Lett. 11, 1999 (2009)
  2. 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)
  3. 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)
  4. Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis: R.A. Mesa; IDrugs 13, 394 (2010)
  5. The JAK-inhibitor ruxolitinib impairs dendritic cell function in vitro and in vivo: A. Heine, et al.; Blood 122, 1192 (2013)
  6. Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348): T. Zhou, et al.; Leukemia 28, 404 (2014)
  7. Tumoricidal effects of the JAK inhibitor Ruxolitinib (INC424) on hepatocellular carcinoma in vitro: G.S. Wilson, et al.; Cancer Lett. 341, 224 (2013)
  8. INCB018424 induces apoptotic cell death through the suppression of pJAK1 in human colon cancer cells: H.J. An, et al.; Neoplasma 61, 56 (2014)
  9. Ruxolitinib is a potent immunosuppressive compound: is it time for anti-infective prophylaxis? A. Heine, et al.; Blood 122, 3843 (2013)
  10. 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)
  11. Ruxolitinib induces autophagy in chronic myeloid leukemia cells: B.G. Bagca, et al.; Tumour Biol. 37, 1573 (2016)
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