Ruxolitinib CAS: 941678-49-5
MF: C17H18N6
MW: 306.37

Ruxolitinib (CAS 941678-49-5)

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Nombres Alternativos: Ruxolitinib is also known as INCB 018424.
Solicitud: Ruxolitinib is a potent Janus-associated kinase (JAK) inhibitor, selective to JAK1, JAK2, and JAK3.
Número de CAS: 941678-49-5
Pureza: ≥98%
Peso Molecular: 306.37
Fórmula Molecular: C17H18N6
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
* En el Certificado de Análisis específico de lote, puede encontrar información específica (como el contenido en agua).
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Ruxolitinib is a JAK inhibitor of JAK1 (IC50 = 2.7 nM), JAK2 (IC50 = 4.5 nM), and JAK3 (IC50 = 322 nM). JAKs, or Janus-associated kinases, are tyrosine kinases found in the cytoplasm that are known to activate the signaling of certain growth factor receptors and cytokines. As a potent ATP mimetic, Ruxolitinib inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC50 = 322 nM). Ruxolitinib can block interleukin-6 (IL-6) signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM). In primary cultures, ruxolitinib preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ polycythemia vera patients (IC50 = 67 nM) versus healthy donors (IC50 > 400 nM).


References

1. Leonard, W.J., and O′Shea, J.J.JAKS AND STATS: Biological implications. Annual Reviews of Immunology 16, 293-322 (1998).
2. Yamaoka, K., Saharinen, P., Pesu, M., et al.The Janus kinases (Jaks). Genome Biol. 5(12), 253 (2004).
3. Verstovsek, S.Therapeutic potential of JAK2 inhibitors. Hematology Am.Soc.Hematol.Educ.Program 2009(1), 636-642 (2009).
4. Quintás-Cardama, A., Vaddi, K., Liu, P., et al.Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: Therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115(15), 3109-3117 (2010).

Apariencia :
Powder
Estado de Materia :
Solid
Solubilidad :
Soluble in DMSO (61 mg/ml at 25° C), ethanol (15 mg/ml) with warming, DMF (~5 mg/ml), water (<1 mg/ml at 25° C), and methanol.
ALMACENAMIENTO :
Store at -20° C
Punto de Fusión :
86-89° C
Punto de ebullición :
~592.6° C at 760 (Predicted)
Densidad :
~1.4 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.75 (Predicted)
Actividad Óptica :
α20D -8.0, c = 0.3 in methanol
IC50 :
JAK1: IC50 = 0.8 nM (human); JAK2: IC50 = 2.8 nM (human); JAK3: IC50 = 10.7 nM (human); Tyk 2: IC50 = 19 nM (human); JAK3/JAK1: IC50 = 23 nM (human)
Datos Ki :
JAK1: Ki= 0.09 nM (human); JAK2: Ki= 0.1 nM (human); Tyk 2: Ki= 0.5 nM (human); JAK3: Ki= 3.2 nM (human)
Valores de pK :
pKa: 11.63 (Predicted), pKb: 3.67 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
PubChem CID :
Número MDL :
MFCD12031592
SMILES :
C1CCC(C1)[[email protected]@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

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PMID: # 32937365  Verma, N.|Vinik, Y.|Saroha, A.|Nair, NU.|Ruppin, E.|Mills, G.|Karn, T.|Dubey, V.|Khera, L.|Raj, H.|Maina, F.|Lev, S.| et al. 2020. Sci Adv. 6:

PMID: # 31992798  Qadir, AS.|Stults, AM.|Murmann, AE.|Peter, ME.| et al. 2020. Sci Rep. 10: 1310.

PMID: # 31391303  2019. Proc. Natl. Acad. Sci. U.S.A. 116: 17399-17408.

PMID: # 30891766  He, Z. et al. 2019. Ann. N. Y. Acad. Sci. 1442: 128-137.

PMID: # 29907868  Ménoret, A.|Buturla, JA.|Xu, MM.|Svedova, J.|Kumar, S.|Rathinam, VAK.|Vella, AT.| et al. 2018. Mucosal Immunol. 11: 1398-1407.

PMID: # 30012499  Mesbahi, Y.|Zekri, A.|Ghaffari, SH.|Tabatabaie, PS.|Ahmadian, S.|Ghavamzadeh, A.| et al. 2018. Eur. J. Pharmacol. 834: 65-76.

PMID: # 30348790  2018. Eur. J. Pharmacol. 834: 65-76.

PMID: # 30247637  2018. Mol. Hum. Reprod. 24: 533-542.

PMID: # 26573834  Tsurutani, N. et al. 2016. Journal of immunology (Baltimore, Md. : 1950). 196: 124-34.

PMID: # 27035543  Jinushi, M. et al. 2016. Viral immunology. 29: 296-306.

Citaciones 1 a 10 de un total de 15
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