LMP744 hydrochloride(Synonyms: MJ-III65 hydrochloride; NSC706744 hydrochloride)

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LMP744 hydrochloride (Synonyms: MJ-III65 hydrochloride; NSC706744 hydrochloride) 纯度: 99.70%

LMP744 hydrochloride (MJ-III65 hydrochloride) 是一种 DNA 嵌和剂,是 拓扑异构酶 1 (Top1) 抑制剂,具有抗肿瘤活性。

LMP744 hydrochloride(Synonyms: MJ-III65 hydrochloride; NSC706744 hydrochloride)

LMP744 hydrochloride Chemical Structure

CAS No. : 308246-57-3

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1 mg ¥3500 In-stock
5 mg ¥9500 In-stock
10 mg ¥15000 In-stock
50 mg ¥45000 In-stock
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生物活性

LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity[1].

IC50 & Target

Top1

 

体外研究
(In Vitro)

The GI50 value of LMP744 (MJ-III-65) for NCI60 cells is 0.1 μM[2].
LMP744 (0.1-5 μM, 3 days) induces dose-dependent accumulation of cells in the S and G2 phases of the cell cycle[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[2]

Cell Line: P388 and P388 Top1-deficient murine leukemia cells.
Concentration: 0.1-100 μM
Incubation Time: 3 days
Result: Induced dose-dependent accumulation of cells in the S and G2 phases of the cell cycle.

体内研究
(In Vivo)

LMP744 (MJ-III-65) (10-50 mg/kg) administered i.v. push once a week for 4 weeks in nude mice moderately actives against human A253 and FaDu tumor xenografts without significant toxicity[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic nude mice (nu/nu, female, 20-25 g, 8-12 weeks old) transplanted with A253 and FaDu human head and neck xenografts[1].
Dosage: 10, 25, or 50 mg/kg/week, 4 weeks
Administration: I.V. push via tail vein
Result: Moderately actived against human A253 and FaDu tumor xenografts without significant toxicity.

Clinical Trial

分子量

488.92

Formula

C24H25ClN2O7

CAS 号

308246-57-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 105 mg/mL (214.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0453 mL 10.2266 mL 20.4532 mL
5 mM 0.4091 mL 2.0453 mL 4.0906 mL
10 mM 0.2045 mL 1.0227 mL 2.0453 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Antony S, et al. Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison. Mol Pharmacol. 2005 Feb;67(2):523-30.

    [2]. Antony S, et al. Bisindenoisoquinoline bis-1,3-{( 5,6-dihydro-5,11-diketo-11H-indeno [1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA intercalator and topoisomerase inhibitor with antitumor activity. Mol Pharmacol. 2006 Sep;70(3):1109-20.

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