BIIB-057

BIIB-057

CAT N°: 17652
Price:

From 80.00 68.00

BIIB-057 is a potent inhibitor of the non-receptor tyrosine kinase Syk (IC50 = 1 nM).{28676} It displays at least 80-fold selectivity for Syk over other kinases. BIIB-057 blocks B cell receptor-mediated cell signaling and activation in whole blood (IC50s = 0.27 and 0.28 µM, respectively), as well as Fc? receptor 1-mediated basophil degranulation (IC50 = 0.15 µM).{28676} It antagonizes chemokine production, cell migration, and survival of chronic lymphocytic leukemia (CLL) cells after B cell receptor activation and synergistically enhances the action of fludarabine (Item No. 14128) in killing CLL cells.{28677,28678} BIIB-057 is orally bioavailable, as it produces dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis.{28676} It also prevents splenomegaly and inhibits non-Hodgkin lymphoma tumor growth in a xenograft model.{28678}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-5-pyrimidinecarboxamide
  • Correlated keywords
    • 1370261-97-4 biochemical inhibitor kinase protein signal transduction intracellular signaling arthritis cancer inflammation BIIB057 inhibit PRT-2607 PRT-062607 1370261-98-5 P50515
  • Product Overview:
    BIIB-057 is a potent inhibitor of the non-receptor tyrosine kinase Syk (IC50 = 1 nM).{28676} It displays at least 80-fold selectivity for Syk over other kinases. BIIB-057 blocks B cell receptor-mediated cell signaling and activation in whole blood (IC50s = 0.27 and 0.28 µM, respectively), as well as Fc? receptor 1-mediated basophil degranulation (IC50 = 0.15 µM).{28676} It antagonizes chemokine production, cell migration, and survival of chronic lymphocytic leukemia (CLL) cells after B cell receptor activation and synergistically enhances the action of fludarabine (Item No. 14128) in killing CLL cells.{28677,28678} BIIB-057 is orally bioavailable, as it produces dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis.{28676} It also prevents splenomegaly and inhibits non-Hodgkin lymphoma tumor growth in a xenograft model.{28678}

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