您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Cephaeline
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Cephaeline
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cephaeline图片
CAS NO:483-17-0
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
吐根酚碱
吐根鹼
产品介绍
Cephaeline 对受保护的原代 CLL 细胞具有高度活性(相对 IC50 为 35nM),并通过抑制 HIF-1α± 和扰乱细胞内氧化还原稳态发挥作用。

产品描述

Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.

体外活性

We compared the transcriptomes of primary CLL cells cocultured or not with protective bone marrow stromal cells (BMSCs) and found that oxidative phosphorylation, mitochondrial function, and hypoxic signaling undergo most significant dysregulation in non-protected CLL cells, with the changes peaking at 6-8 h, directly before induction of apoptosis. A subset of CLL patients displayed a gene expression signature resembling that of cocultured CLL cells and had significantly worse progression-free and overall survival. To identify drugs blocking BMSC-mediated support, we compared the relevant transcriptomic changes to the Connectivity Map database. Correlation was found with the transcriptomic signatures of the cardiac glycoside ouabain and of the ipecac alkaloids emetine and Cephaeline. These compounds were highly active against protected primary CLL cells (relative IC50's 287, 190, and 35 nM, respectively) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis. We tested emetine in a murine model of CLL and observed decreased CLL cells in peripheral blood, spleen, and bone marrow, recovery of hematological parameters and doubling of median survival (31.5 vs. 15 days, P = 0.0001).

Cas No.

483-17-0

分子式

C28H38N2O4

分子量

466.61

别名

吐根酚碱;吐根鹼

储存和溶解度

Ethanol:33.33 mg/mL (71.43 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years