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SJG-136

(Synonyms: NSC-694501)

目录号: PL04125 纯度: ≥98%

SJG-136 是一种有效的 DNA 交联剂 (DNA crosslinker)，与 pBR322 DNA 交联的 XL50 值为 45 nM。SJG-136 具有抗肿瘤作用。

CAS No. :232931-57-6

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中文名称	SJG-136
中文别名	SJG-136;(11AS,11'AS)-8,8'-[1,3-丙二基双(氧基)]双[1,2,3,11A-四氢-7-甲氧基-2-亚甲基-5H-吡咯并[2,1-C] [1,4]苯并二氮杂-5-酮]
英文名称	SJG-136
英文别名	SJG-136;(6aS)-3-[3-[[(6aS)-2-methoxy-8-methylidene-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-2-methoxy-8-methylidene-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one;NSC 694501;NSC-694501;SJG136;(6aS)-3-[3-[[(6aS)-2-methoxy-8-methylene-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-2-methoxy-8-methylene-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one;NSC-D694501;SP-2001;UP-2001;(11aS,11'aS)-8,8'-[1,3-Propanediylbis(oxy)]bis[1,2,3,11a-tetrahydro-7-methoxy-2-methylene-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one;UP 2001;SJG 136;KT0ZQ64X1A;NSC694501
Cas No.	232931-57-6
分子式	C₃₁H₃₂N₄O₆
分子量	556.61
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

SJG-136 是一种有效的 DNA 交联剂 (DNA crosslinker)，与 pBR322 DNA 交联的 XL₅₀ 值为 45 nM。SJG-136 具有抗肿瘤作用。

生物活性

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

性状

Solid

IC50 & Target[1][2]

Pyrrolobenzodiazepines

体外研究(In Vitro)

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

体内研究(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. 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]. 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.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (59.88 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

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。

SJG-136

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