AZD1208

AZD1208

产品参数

货号 规格 操作
A127698-25mg 咨询
A127698-5mg 咨询
A127698-100mg 咨询
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服务地域:全国

属性:产地:上海; 品牌:阿拉丁 ;货期:现货

上海阿拉丁生化科技股份有限公司

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产品描述产品描述
  • 分子式 C21H21N3O2S
  • 分子量379.48
  • Beilstein号
  • EC号
  • MDL号
  • PubChem编号

属性

溶解性 DMSO
存贮条件 储存温度-20°C

描述

产品介绍 AZD1208是口服活性的PIM高选择性抑制剂,对Pim1, Pim2, 和 Pim3的IC50分别为5 nM, 25 nM 和 16 nM。
生化机理

Description:
IC50 Value:
AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases and is currently undergoing Phase I testing and dose escalation studies in AML.
AZD1208 suppresses the growth of MOLM 16 and KG 1 xenograft tumors in vivo in a dosedependent manner. Furthermore, AZD1208 leads to potent inhibition of colony development of primary AML cells from bone marrow aspirates and downregulates the phosphorylation of PIM goals. AZD1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of PIM1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture.
 

别名 AZD 1208;AZD-1208;(5Z)-5-[[2-[(3R)-3-氨基-1-哌啶基][1,1'-联苯]-3-基]亚甲基]-2,4-噻唑烷二酮;AZD 1208;AZD-1208;;(5Z)-5-[[2-[(3R)-3-Amino-1-piperidinyl][1,1'-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione
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