3-deazaneplanocin A HCl - CAS:120964-45-6 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	3-deazaneplanocin A HCl
英文名称:	3-deazaneplanocin A HCl
别名:	3-去氮腺嘌呤A (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol;hydrochloride
CAS No:	120964-45-6	分子式:	C₁₂H₁₄N₄O₃^.HCl	分子量:	298.73
CAS No:	120964-45-6
分子式:	C₁₂H₁₄N₄O₃^.HCl
分子量:	298.73
MDL:	MFCD18782644	EINEC:	617989
EINEC:	617989

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

D10090 3-deazaneplanocin A HCl ≥98%(HPLC) (psaitong)

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包装规格：

1mg 5mg 25mg in glass bottle

溶解性：

溶于DMSO(59mg/mL)和水。

产品描述：

基本信息

产品编号：D10090
产品名称：3-deazaneplanocin A HCl
CAS:	120964-45-6	储存条件	粉末	-20℃	四年

分子式：	C12H14N4O3.HCl		溶于液体	-80℃	六个月
分子量：	298.73			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	59mg/mL (197.5mM)
		Ethanol	Insoluble
		Water	59mg/mL (197.5mM)
	体内（现配现用）	Saline	30mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.3475mL	16.7375mL	33.4750mL
5mM	0.6695mL	3.3475mL	6.6950mL
10mM	0.3348mL	1.6738mL	3.3475mL
50mM	0.0670mL	0.3348mL	0.6695mL

生物活性

产品描述	一处EZH2(组蛋白甲基转移酶)抑制剂。
靶点/IC50	S-adenosylhomocysteine hydrolase
靶点/IC50	50pM(Ki)
体外研究	3-Deazaneplanocin A is a potent histone methyltransferase EZH2 inhibitor.Treatment of OCI-AML3 cells with 3-Deazaneplanocin A (1.0μM) results in a significant increase in accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle (P<0.05).Treatment with 3-Deazaneplanocin A (200nM to 2.0μM) for 48 hours,dose dependently,inhibits colony growth of OCI-AML3 and HL-60 cells.3-Deazaneplanocin A reduces the expression of EZH2,especially after 72 hours (e.g.48%,32% and 36% reduction of EZH2 in PANC-1,MIA-PaCa-2 and LPc006 cells,respectively).3-Deazaneplanocin A shows minimal growth inhibition in PANC-1 cells.More than 50% of these cells are still growing after exposure at the highest concentration (20μM).MIA-PaCa-2 and LPc006 cells are much more sensitive,with IC0 values of 1±0.3 and 0.1±0.03μM,respectively.3-Deazaneplanocin A causes dose-dependent inhibition of cell proliferation of NSCLC cell lines,and the IC0 values range from 0.08 to 0.24μM.
体内研究	The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher,if treated with 3-Deazaneplanocin A and Panobinostat (PS) compare to treatment with PS,3-Deazaneplanocin A,or vehicle alone (P<0.05).Median survival is as follows:control,36 days;PS,42 days;3-Deazaneplanocin A, 43 days;and 3-Deazaneplanocin A plus PS,52 days.There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day).Administration of 20mg/kg 3-Deazaneplanocin A not only markedly reduces the relative weight of the rats compare to the initial weight (−2.0%,−4.9% and−1.2%) in the first three days post-treatment,but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose.

推荐实验方法(仅供参考)

激酶实验：

S-腺苷同型半胱氨酸水解酶活性测定

AdoHcyase检测的反应混合物有0.5mL,50mM 磷酸钾 (pH 7.6),5mM 二硫苏糖醇,1mM EDTA,10%甘油，和酶。L-[8-14C]AdoHcy用作底物，包括5个单位小牛肠腺苷脱氨酶。加入100μL 5M甲酸终止反应，然后反应混合物加到SP-Sephadex C-25柱(0.8×2.5cm)中,在 0.1M 甲酸中平衡。每个试管使用0.5mL 0.1M甲酸进行漂洗。3.5mL 0.1M甲酸加到闪烁瓶中，从从柱中洗脱形成[14C]肌苷。加入10mL闪烁液后测定放射性。使用的酶量约为105pU,或75ng纯化的酶。在37°C下，1分钟内形成1pmol产物需要的酶量为一个单位。

细胞实验:

AML HL-60 cells are obtained and maintained.OCI-AML-3 cells are cultured in α minimum essential medium with 10% fetal bovine serum,1% penicillin/streptomycin,and 1% nonessential amino acids.To analyze synergism between 3-Deazaneplanocin A and PS in inducing apoptosis,cells are treated with 3-Deazaneplanocin A (100-750nM) and PS (5-20nM) at a constant ratio for 48 hours.The percentage of apoptotic cells is determined by flow cytometry.The combination index (CI) for each drug combination is obtained by median dose effect of Chou and Talalay,using the CI equation within the commercially available software Calcusyn.

动物实验:

Rats

Male wistar rats are used.The acute toxicity study is carried out to determine the NOAEL of 3-Deazaneplanocin A in rats.In total,20 rats are divided into 4 groups of five each.Three groups are intravenously administered 20,15,10mg/kg body weight (BW) 3-Deazaneplanocin A solution by the tail vein.The remaining group is given physiological saline (0.9% NaCl saline) as the control group.Then,the NOAEL of free 3-Deazaneplanocin A is determined,depending on the following endpoint parameters obtained.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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