A potent

BIIB-057 – 5 mg

Brand:
Cayman
CAS:
1370261-96-3
Storage:
-20
UN-No:
Non-Hazardous - /

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 Fcɛ 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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Description

A potent, selective, orally bioavailable inhibitor of Syk (IC50 = 1 nM); blocks B cell receptor-mediated cell signaling and activation in whole blood (IC50s = 0.27 and 0.28 µM, respectively); inhibits inflammation and tumor growth in animal models of rheumatoid arthritis and non-Hodgkin lymphoma, respectively

Formal name: 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-5-pyrimidinecarboxamide

Synonyms:  P505-15|PRT062607|PRT2607

Molecular weight: 393.5

CAS: 1370261-96-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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