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AdipoGen Life Sciences
Ruxolitinib (free base)
80
CHF
CHF 80.00
In stock
AG-CR1-3624-M0055 mgCHF 80.00
AG-CR1-3624-M02525 mgCHF 180.00
AG-CR1-3624-M100100 mgCHF 360.00
| Product Details | |
|---|---|
| Synonyms | INCB018424; INC 424 |
| Product Type | Chemical |
| Properties | |
| Formula |
C17H18N6 |
| MW | 306.4 |
| CAS | 941678-49-5 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO or ethanol. Insoluble in water. |
| Identity | Determined by 1H-NMR and MS. |
| InChi Key | HFNKQEVNSGCOJV-OAHLLOKOSA-N |
| Smiles | N#CC[C@H](C1CCCC1)N1C=C(C=N1)C1=NC=NC2=C1C=CN2 |
| 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. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- 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. It is investigated against the spread of the SARS-CoV-2 (COVID-19).
Product References
- 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)
- The Human Liver-Expressed Lectin CD302 Restricts Hepatitis C Virus Infection: B. Reinecke, et al.; J. Virol. 96, e0199521 (2022)
- The matrix metalloproteinase ADAM10 supports hepatitis C virus entry and cell-to-cell spread via its sheddase activity: B. Carriqui-Madronal, et al. PLoS Pathogen 19, e1011759 (2023)
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