LMP744 hydrochloride

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CAS NO:

308246-57-3

MJ-III65 hydrochloride
NSC706744 hydrochloride

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。

生物活性

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

IC₅₀& Target

Top1

体外研究
(In Vitro)

The GI₅₀value 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 G₂phases of the cell cycle^[2].

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 G₂phases 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].

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

性状

Solid

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。