SJG-136, DNA 交联剂

CAS: 232931-57-6 货号: S656456 分子式: C31H32N4O6 分子量: 556.61
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
S656456-1ml
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¥6,000.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


SJG-136 is a DNA cross-linking agent, with an XL 50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity.

In Vitro

SJG-136 (dimer 5) is a DNA cross-linking agent, with an XL 50 (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 (IC 50 , 22.5 pM), A2780cisR (IC 50 , 24 pM), CH1 (IC 50 , 0.12 nM), CH1cisR (IC 50 , 0.6 nM), and SKOV-3 (IC 50 , 9.1 nM). SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI 50 values ranging from 0.33 - >100 nM after a 1 h exposure, and <0.03 - 17.33 nM following continuous exposure. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal administration

A homogenous suspension of 5 × 10 6 exponentially growing canine melanoma cells in serum free RPMI 1640 tissue culture medium is injected subcutaneously into CD1 Nu/Nu immunocompromised female mice . The mice are divided into five groups of ten mice, with equivalent mean tumour volumes for each group. SJG-136 is given intravenously into the tail vein to four of these groups and vehicle control is administered to the fifth group. SJG-136 injections are prepared in 0.9 % NaCl and 1 % DMSO vehicle . Animals are weighed prior to the injection to determine the volume of SJG-136 required (0.1 mL/10 g body weight) which is given IV in the tail vein. Control group mice are given an IV injection of the vehicle solution; mice in groups one and two are given a single treatment of SJG-136, 0.15 mg/kg and 0.30 mg/kg respectively; mice in groups four and five are given 0.15 mg/kg and 0.30 mg/kg respectively, every seven days for a total of three treatments . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Pyrrolobenzodiazepines

规格

规格或纯度
10mM in DMSO
英文名称
SJG-136
生化机理
SJG-136 是一种 DNA 交联剂,对 pBR322 DNA 的 XL 50 为 45 nM。SJG-136 具有很强的抗肿瘤活性。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
交联剂
作用机制
DNA 交联剂
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C=C2C(=C1)C(=O)N3CC(=C)C[C@H]3C=N2)OCCCOC4=C(C=C5C(=C4)N=C[C@@H]6CC(=C)CN6C5=O)OC
分子量
556.61

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高级数据

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