AZD1208
目录号: PL09861 纯度: ≥99%
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
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
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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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