AZD1208

目录号: PL09861 纯度: ≥99%
AZD1208 是一种有效的,具有口服活性的,具有高度选择性的 PIM 抑制剂。
CAS No. :1204144-28-4
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中文名称
AZD1208
中文别名
(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;AZD1208 抑制剂
英文名称
AZD1208
英文别名
AZD1208;(R,Z)-5-((2-(3-Aminopiperidin-1-yl)-[1,1'-biphenyl]-3-yl)methylene)thiazolidine-2,4-dione;AZD-?1208;Azd-1208;AZD 1208;S98NFM1378;GTPL7698;AK174910;(5Z)-5-[[2-[(3R)-3-aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione;(5Z)-5-({2-[(3R)-3-Aminopiperidin-1-yl]-3-phenylphenyl}methylidene)-1,3-thiazolidine-2,4-dione;AOB87151;s7104;2236AH;BDBM50387298;5-[[2-[(3R)-3-Aminopiperidin-1-yl]biphenyl-3-yl]methylidene]-1,3-thiazolidine-2,4-dione;BDB
Cas No.
1204144-28-4
分子式
C21H21N3O2S
分子量
379.48
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
AZD1208 是一种有效的,具有口服活性的,具有高度选择性的 PIM 抑制剂。
产品详情
AZD1208 是一种有效的,具有口服活性的,具有高度选择性的 PIM 抑制剂。
生物活性
AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.
性状
Solid
体外研究(In Vitro)
AZD1208 shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI50 values less than 100 nM. AZD1208 (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cell at 1 μM. AZD1208 induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle. The combination of AZD1208 and AZD2014 rapidly activates AMPKα, a negative regulator of translation machinery through mTORC1/2 signaling in AML cells; profoundly inhibits AKT and 4EBP1 activation; and suppresses polysome formation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Dakin LA, et al. Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604.
[2]. Kreuz S, et al. Loss of PIM2 enhances the anti-proliferative effect of the pan-PIM kinase inhibitor AZD1208 in non-Hodgkin lymphomas. Mol Cancer. 2015 Dec 8;14:205.
溶解度数据
In Vitro: DMSO : 50 mg/mL (131.76 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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