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M344

目录号 M3395 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


M344是一种有效的HDAC抑制剂,IC50为100 nM,可以诱导细胞分化。

M344结构式

别名:D 237; MS 344

规格 价格 库存状态
5mg ¥ 780 中国库存现货
10mg ¥ 1235 中国库存现货
50mg ¥ 5460 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

M344 shows a potent inhibition activity against histone deacetylase with IC50 of 100 nM. M344 produces a more significant effect on cell proliferation than on cell differentiation in MEL DS19 cells. M344 shows cell toxicity at concentrations above 10 μM, while a maximum of only 20% of the surviving cell population are induced to differentiate. In vitro, M344 produces the significant anti-proliferative effects on the endometrial cancer cell line Ishikawa and the ovarian cancer cell line SK-OV-3 with EC50 of 2.3 μM and 5.1 μM, respectively. While the normal human endometrial epithelial cells shows little sensitivity to M344. In addition, M344 also decreases proportion of cells in the S-phase, increases proportion in the G0/G1 phases of the cell cycle, induces apoptosis and decreases the transmembrane potential of mitochondria. M344 show the anti-proliferative activities against embryonal nervous system tumor cells including medulloblastoma cells (D341 Med, Daoy) and neuroblastoma cells (CH-LA 90,SHSY-5Y ) with GI50 of 0.65 μM, 0.63 μM, 0.63 μM and 0.67 μM, respectively.M344 (5 μM ) in combination with cisplatin (10 μg/mL) results increased induction of ATF3 and shows enhanced cytotoxic effects than cisplatin alone in a panel of human derived cancer cell lines, such as MCF-7, PC3, SK-OV3, and A549.

产品使用成果展示
数据来源 Cell Death Dis (2018). Figure 1. M344
方法 cell viability assay
细胞系/动物模型 T-ALL cells
浓度 1 μM
处理时间 24 and 48 h
实验结果 Compared with the single treatment (Fig. 1a–c), the combination of vorinostat and QC significantly decreased cell viability.
实验参考
体外实验*
细胞系 MEL DS19 cells
方法 Maintaining MEL DS19 cells (murine erythroleukemia cells) in D-MEM containing 100 units/mL penicillin G sodium and 100 μg/mL streptomycin sulfate supplemented with 10% fetal bovine serum at 37 °C in a 5% CO2 atmosphere. To test M344 for potential to induce cell differentiation, log-phase cells with a population doubling time of 11−13 hours are used. Preparing Serial dilutions of M344 in 24-well plates using 1 mL of D-MEM/well. If M344 are dissolved in DMSO, control wells contains the same amount of solvent (generally 2 μL/mL of medium). Subsequently, adding the cell suspension to the wells. After 72 hours the experiment is evaluated. Using a Casy 1 TTC flow cytometer to counte cell numbers. With the solvent control , expressing the proliferation of treated cells as percent proliferation in comparison. Differentiated MEL cells accumulate hemoglobin. Therefore, the induction of cell differentiation is determined by benzidine staining according to the literature. To 100 μL of cell suspension is added 10 μL of a 0.4% solution of benzidine in 12% acetic acid which contains 2% H2O2. Within 5 minutes hemoglobin-containing cells stains blue.Under the microscope in a hemocytometer ,counting Benzidine-positive and -negative cells , and calculating the percentage of positive cells . Testing M344 first at 10 μM and 50 μM final concentration. A range of concentrations is chosen for a dose−response analysis according to activity/toxicity profile,.
浓度 0 to 50 μM
处理时间 72 hours

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
动物模型
配制
剂量
给药处理

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 307.39
分子式 C16H25N3O3
CAS号 251456-60-7
溶解性(25°C) DMSO 55 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.2532 mL 16.266 mL 32.532 mL
5 mM 0.6506 mL 3.2532 mL 6.5064 mL
10 mM 0.3253 mL 1.6266 mL 3.2532 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Claude-Henry Volmar, et al. M344 promotes nonamyloidogenic amyloid precursor protein processing while normalizing Alzheimer's disease genes and improving memory

[2] L Jin, et al. Histone deacetylase inhibitor M344 significantly improves nuclear reprogramming, blastocyst quality, and in vitro developmental capacity of cloned pig embryos

[3] No authors listed. Gynecol Oncol. Retraction notice to "M344 is a novel synthesized histone deacetylase inhibitor that induces growth inhibition, cell cycle arrest, and apoptosis in human endometrial cancer and ovarian cancer cells" [Gynecol. Oncol. 101 (2006) 108-113]

[4] Angie Yeung, et al. HDAC inhibitor M344 suppresses MCF-7 breast cancer cell proliferation

[5] Noriyuki Takai, et al. M344 is a novel synthesized histone deacetylase inhibitor that induces growth inhibition, cell cycle arrest, and apoptosis in human endometrial cancer and ovarian cancer cells

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关键词:M344, D 237; MS 344, M344供应商, HDAC抑制剂, 购买M344, M344溶解度, M344结构式








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