您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > SJG-136(NSC-694501)
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:
 
SJG-136(NSC-694501)
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。
SJG-136(NSC-694501)图片
CAS NO:232931-57-6
规格:98%
分子量:556.61
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议

产品介绍
SJG-136是一种有效的DNA交联剂(DNAcrosslinker),与pBR322DNA交联的XL50值为45nM;SJG-136具有抗肿瘤作用。
CAS:232931-57-6
分子式:C31H32N4O6
分子量:556.61
纯度:98%
存储:Store at -20°C

Background:

SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA; SJG-136 has potent antitumor activity.


SJG-136 (dimer 5) is a DNA cross-linking agent, with an XL50 (concentration of agent required for 50% cross-linking of pBR322 DNA) of 45 nM for pBR322 DNA. SJG-136 is cytotoxic to ovarian cell lines, such as A2780 (IC50, 22.5 pM), A2780cisR (IC50, 24 pM), CH1 (IC50, 0.12 nM), CH1cisR (IC50, 0.6 nM), and SKOV-3 (IC50, 9.1 nM)[1]. SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI50 values ranging from 0.33 - >100 nM after a 1 h exposure, and<0.03 - 17.33 nM following continuous exposure[2].


SJG-136 shows more potent antitumor effect against CMeC-1 tumour at 0.30 mg/kg than 0.15 mg/kg either as a single dose or administered once a week for three weeks via dosed intravenously in mice. SJG-136-induced H2AX phosphorylation shows good correspondence, but less sensitivity, than measurement of foci[2].


[1]. Gregson SJ, et al. Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity. J Med Chem. 2001 Mar 1;44(5):737-48. [2]. Mellinas-Gomez M, et al. Activity of the DNA minor groove cross-linking agent SG2000 (SJG-136) against canine tumours. BMC Vet Res. 2015 Aug 19;11:215.