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| | 5-[[2-[(3R)-3α-アミノ-1-ピペリジニル]-3-ビフェニリル]メチレン]チアゾリジン-2,4-ジオン 製品概要 |
| 化学名: | 5-[[2-[(3R)-3α-アミノ-1-ピペリジニル]-3-ビフェニリル]メチレン]チアゾリジン-2,4-ジオン | | 英語化学名: | AZD-1208 | | 别名: | AZD 1208;AZD1208;AZD-1208;(5Z)-5-[[2-[(3R)-3-aMino-1-piperidinyl][1,1'-biphenyl]-3-yl]Methylene]-2,4-thiazolidinedione;(5Z)-5-[[2-[(3R)-3-Amino-1-piperidinyl][1,1'-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione AZD1208;(R,Z)-5-((2-(3-aminopiperidin-1-yl)biphenyl-3-yl)methylene)thiazolidine-2,4-dione;(R,Z)-5-((2-(3-aMinopiperidin-1-yl)-[1,1'-biphenyl]-3-yl)Methylene)thiazolidine-2,4-dione;AZD1208 >=95% | | CAS番号: | 1204144-28-4 | | 分子式: | C21H21N3O2S | | 分子量: | 379.48 | | EINECS: | | | カテゴリ情報: | Inhibitors;JAK;STAT;JAK/STAT | | Mol File: | 1204144-28-4.mol | ![5-[[2-[(3R)-3α-アミノ-1-ピペリジニル]-3-ビフェニリル]メチレン]チアゾリジン-2,4-ジオン](CAS/20150408/GIF/1204144-28-4.gif) |
| | 5-[[2-[(3R)-3α-アミノ-1-ピペリジニル]-3-ビフェニリル]メチレン]チアゾリジン-2,4-ジオン 物理性質 |
| 融点 | >220°C (dec.) | | 比重(密度) | 1.307±0.06 g/cm3(Predicted) | | 貯蔵温度 | Hygroscopic, -20°C Freezer, Under inert atmosphere | | 溶解性 | DMSO (Slightly) | | 酸解離定数(Pka) | 7.39±0.20(Predicted) | | 外見 | Solid | | 色 | Off-White to Pale Yellow |
| | 5-[[2-[(3R)-3α-アミノ-1-ピペリジニル]-3-ビフェニリル]メチレン]チアゾリジン-2,4-ジオン Usage And Synthesis |
| 使用 | AZD1208 is a potent, and orally available Pim kinase inhibitor. | | 生物活性 | upregulation of pim kinases has been observed in several types of leukemias and lymphomas. pim-1, -2, and -3 promote cell proliferation and survival downstream of cytokine and growth factor signaling pathways. azd1208 is a potent, highly selective, and orally available pim kinase inhibitor. | | in vitro | azd1208 inhibited the growth of 5 of 14 acute myeloid leukemia (aml) cell lines tested. in molm-16 cells, azd1208 also causes cell cycle arrest and apoptosis, accompanied by a dose-dependent reduction in phosphorylation of bcl-2 antagonist of cell death [1]. | | in vivo | azd1208 inhibits the growth of kg-1a and molm-16 xenograft tumors in vivo with a clear pk/pd relationship. treatment with 10 mg/kg or 30 mg/kg of azd1208 led to an 89% tumor growth inhibition or slight regression, respectively [1]. | | target | Pim1 | | IC 50 | 0.4 nm for pim-1, 5.0 nm for pim-2, and 1.9 nm for pim-3 | | 貯蔵 | Store at -20°C | | 参考文献 | [1] keeton ek, mceachern k, dillman ks, palakurthi s, cao y, grondine mr, kaur s, wang s, chen y, wu a, shen m, gibbons fd, lamb ml, zheng x, stone rm, deangelo dj, platanias lc, dakin la, chen h, lyne pd, huszar d. azd1208, a potent and selective pan-pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia. blood. 2014;123(6):905-13. |
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