PRT062607 (P505-15)

A potent, orally bioavailable Syk inhibitor

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库存: 现货

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5mg

￥1125.00

900.00

- +
10mg

￥1637.00

1310.00

- +
50mg

￥5812.00

4650.00

- +

已选 0 种 0 瓶

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货号: ajce47880
CAS: 1370261-96-3
别名: 2-[[(1R,2S)-2-氨基环己基]氨基]-4-[[3-(2H-1,2,3-三唑-2-基)苯基]氨基]-5-嘧啶甲酰胺,P505-15; PRT-2607; BIIB-057
分子式: C19H23N9O
分子量: 393.45
纯度: >98%
溶解度: DMF: 50 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 25 mg/ml,Ethanol: 10 mg/ml
储存: Store at -20°C
库存: 现货

Background

BIIB-057 is a potent inhibitor of the non-receptor tyrosine kinase Syk (IC₅₀ = 1 nM).¹ 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 ?M, respectively), as well as Fc? receptor 1-mediated basophil degranulation (IC₅₀ = 0.15 ?M).¹ 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 in killing CLL cells.^2,3 BIIB-057 is orally bioavailable, as it produces dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis.¹ It also prevents splenomegaly and inhibits non-Hodgkin lymphoma tumor growth in a xenograft model.³

1.Coffey, G., DeGuzman, F., Inagaki, M., et al.Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritisJ. Pharmacol. Exp. Ther.340(2)350-359(2012) 2.Hoellenriegel, J., Coffey, G.P., Sinha, U., et al.Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migrationLeukemia26(7)1576-1583(2012) 3.Spurgeon, S.E., Coffey, G., Fletcher, L.B., 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 leukemiaJ. Pharmacol. Exp. Ther.344(2)378-387(2015)