3-去氮腺嘌呤A盐酸盐|120964-45-6|(3-去氮腺嘌呤A盐酸盐; DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride)-陌孚医药/Medlife

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3-去氮腺嘌呤A盐酸盐 (Synonyms: 3-去氮腺嘌呤A盐酸盐; DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride)

目录号: PC15837 纯度: ≥98%

CAS No. :120964-45-6

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中文名称	3-去氮腺嘌呤A盐酸盐
中文别名	3-去氮腺嘌呤A;(1S,2R,5R)-5-(4-氨基-1H-咪唑并[4,5-c]吡啶-1-基)-3-(羟基甲基)-3-环戊烯-1,2-二醇盐酸盐
英文名称	3-deazaneplanocin A HCl
英文别名	3-Cyclopentene-1,2-diol, 5-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)-, hydrochloride (1:1), (1S,2R,5R)-;3-Deazaneplanocin A Hydrochloride;3-Deazaneplanocin A;3-deazaneplanocin A (DZNeP) HCl;3-Deazaneplanocin A (hydrochloride);3-DEAZANEPLANOCIN HCL;3-Deazaneplanocin hydrochloride;CS-0870;HY-12186;NSC 617989 hydrochloride;SureCN4304150;(-)-1-[(1R,4R,5S)-3-(Hydroxymethyl)-4,5-dihydroxy-2-cyclopenten-1-yl]4-aminoimidazo[4,5-c]pyridine hydrochloride;DZNep hydrochloride;1H-Imidazo[4,5-c]pyridine, 3-cyclopentene-1,2-diol deriv.;NSC 617989 HCl;3-deazaneplanocin A HCl;Histone Methyltransferase EZH2 Inhibitor, DZNep;DZNep;3-Deazaneplanocin A (DZNep) hydrochloride;3-Deazaneplanocin, HCl salt;C12H14N4O3.ClH;2161AH;s7120;A13947;(1S,2R,5R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-e
Cas No.	120964-45-6
分子式	C₁₂H₁₅ClN₄O₃
分子量	298.73
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性	3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities.
性状	Solid
体外研究(In Vitro)	3-Deazaneplanocin A (DZNep) hydrochloride is a potent histone methyltransferase EZH2 inhibitor. Treatment of OCI-AML3 cells with 3-Deazaneplanocin A (1.0 μM) 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 (200 nM to 2.0 μM) for 48 hours, dose dependently, inhibits colony growth of OCI-AML3 and HL-60 cells. 3-Deazaneplanocin A (DZNep) hydrochloride 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 (DZNep) hydrochloride shows minimal growth inhibition in PANC-1 cells. More than 50% of these cells are still growing after exposure at the highest concentration (20 μM). MIA-PaCa-2 and LPc006 cells are much more sensitive, with IC₀ values of 1.0±0.3 and 0.10±0.03 μM, respectively. 3-Deazaneplanocin A (DZNep) hydrochloride causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC₀ values range from 0.08 to 0.24 μM. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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 (DZNep) and LBH589 (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 20 mg/kg 3-Deazaneplanocin A (DZNep) 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. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature or refrigerated transportation.
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)
参考文献	[1]. Fiskus W, et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor LBH589 against human AML cells. Blood, 2009, 114(13), 2733-2743. [Information] [2]. Avan A, et al. Molecular mechanisms involved in the synergistic interaction of the EZH2 inhibitor 3-deazaneplanocin A with LY 188011 in pancreatic cancer cells. Mol Cancer Ther. 2012 Aug;11(8):1735-46. [Information] [3]. Kikuchi J, et al. Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells. Lung Cancer. 2012 Nov;78(2):138-43. [Information] [4]. Sun F, et al. Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus?. Eur J Pharm Sci. 2015 Sep 18;77:290-302. [Information] [5]. Noriko Uchiyama, et al. Aristeromycin and DZNeP cause growth inhibition of prostate cancer via induction of mir-26a. Eur J Pharmacol. 2017 Oct 5;812:138-146. [Information] [6]. Robert O Baker, et al. Potential antiviral therapeutics for smallpox, monkeypox and other orthopoxvirus infections. Antiviral Res. 2003 Jan;57(1-2):13-23. [Information]

溶解度数据

体外研究:

H₂O : 50 mg/mL (167.38 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3475 mL	16.7375 mL	33.4750 mL
5 mM	0.6695 mL	3.3475 mL	6.6950 mL
10 mM	0.3348 mL	1.6738 mL	3.3475 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 50 mg/mL (167.38 mM); Clear solution; Need ultrasonic

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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。

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