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AZD1208
产品别名
1204144-28-4
AZD1208
AZD-1208
(R,Z)-5-((2-(3-Aminopiperidin-1-yl)biphenyl-3-yl)methylene)thiazolidine-2,4-dione
(5Z)-5-[[2-[(3R)-3-Amino-1-piperidinyl][1,1′-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione
AZD 1208
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C21H21N3O2S |
| Molecular weight | 379.48 |
| MDL number | MFCD25976757 |
| Biochem/physiol Actions【生化/生理作用】 | AZD1208 is an orally available, potent ATP-competitive pan-Pim kinase inhibitor (Pim-1/-2/-3 Ki = 0.1/1.92/0.4 nM; Pim-1/-2/-3 IC50 = 0.4/5.0/1.9 nM with [ATP] = Km; Pim-1/-2/-3 IC50 = 2.6/164/17 nM with [ATP] = 5 mM) wtih high target selectivity (by binding assay with a 442-kinase panel). AZD1208 exhibits selective antiproliferation potency against high Pim-1/-2-expressing AML cultures (GI50 in 72 h = 20 nM/MOLM-16, 60 nM/EOL-1, 300 nM/Kasumi-3, 600 nM/KG-1a, 900 nM/MV4-11) and displays in vivo efficacy against MOLM-16 xenograft tumor growth in mice (by 89% or 100%, respectively, with 10 or 30 mg/kg/day p.o.) |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | −20℃ |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
