Cat. No. Name Size Price Add Cart
KI2368PRT062607 (P505-15, BIIB057) HCl5 mg$332
PRT062607 (P505-15, BIIB057) HCl25 mg$1114

Chemical Characteristic

Product NamePRT062607 (P505-15, BIIB057) HCl
SynonymsN/A
CAS No.1370261-97-4
Molecular Weight 429.91
FormulaC19H23N9O.HCl
Chemical Name4-((3-(2H-1,2,3-triazol-2-yl)phenyl)amino)-2-(((1R,2R)-2-aminocyclohexyl)amino)pyrimidine-5-carboxamide hydrochloride
Smilesc1(nc(c(cn1)C(=O)N)Nc1cc(ccc1)n1nccn1)NC1[C@H](CCCC1)N Cl
Chemical Structure

Biological activities

PRT062607 is a novel, highly selective, and orally bioavailable small molecule spleen tyrosine kinase (SYK) inhibitor with an IC50 of 1 nM. PRT062607 inhibits SYK-mediated B-cell receptor (BCR) signaling and decreases cell viability in non-Hodgkin lymphoma (NHL) and chronic lymphocytic leukemia (CLL).[1] In human whole blood, PRT062607 potently inhibits BCR-mediated B cell signaling and activation with IC50s of 0.27 and 0.28 mM, respectively. PRT062607 inhibits Fcε receptor 1 (FcεRI) -mediated basophil de-granulation with an IC50 of 0.15 mM.[2] Oral administration of PRT062607 in mice prevents BCR-mediated splenomegaly and significantly inhibits NHL tumor growth in a xenograft model.[1]

References

[1] Spurgeon SE, et al. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013, 344(2): 378-387.
[2] Coffey G, et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012, 340(2): 350-359.

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