Eflornithine (MDL-71782) hydrochloride hydrate

For research use only. Not for use in humans.

目录号:S4582 别名: Difluoromethylornithine hydrochloride hydrate, DFMO hydrochloride hydrate, RMI-71782 hydrochloride hydrate, α-difluoromethylornithine hydrochloride hydrate 中文名称:依氟鸟氨酸盐酸盐一水合物

Eflornithine (MDL-71782) hydrochloride hydrate Chemical Structure

CAS No. 96020-91-6

Eflornithine (Difluoromethylornithine, DFMO, MDL-71782, RMI-71782, α-difluoromethylornithine) hydrochloride hydrate 通过对鸟氨酸脱羧酶的不可逆抑制作用,抑制多胺生物合成。它是一种化疗保护剂,可阻止血管生成。其生物半衰期为8小时。

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RMB 794.81 现货
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客户使用Selleck生产的Eflornithine (MDL-71782) hydrochloride hydrate发表文献3篇:

质量管理及产品安全说明书

Decarboxylase抑制剂选择性比较

生物活性

产品描述 Eflornithine (Difluoromethylornithine, DFMO, MDL-71782, RMI-71782, α-difluoromethylornithine) hydrochloride hydrate 通过对鸟氨酸脱羧酶的不可逆抑制作用,抑制多胺生物合成。它是一种化疗保护剂,可阻止血管生成。其生物半衰期为8小时。
靶点
Orn decarboxylase [2]
体外研究

用α-difluoromethyl-Orn处理BY2细胞,抑制其过氧化氢的产生,但并没有发生程序性细胞死亡[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
J774.1 NFz6cJNCdnSrdIL5dIFvd3OxbXHsJIF{e2G7 NGf2bXI1QCCqcoO= M{DP[GFvfGm2conwZY5we2:vYXygZYN1cX[rdImgZYdicW6|dDDUdplx[W6xc3;tZUBjenWlZXmgZpJ2[2WrIGTDNlIyKGmwZnXjeIVlKGmwIH3veZNmKEp5N{SuNUBk\WyuczDh[pRmeiB2ODDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVAhRSB{Mj65JO69VS5? NH\sRpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkO3OlA4Oid-MkKzO|YxPzJ:L3G+
A673 NWLhfHU4eUiWUzDhd5NigQ>? NHztd5FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 NHXKWoNyUFSVIHHzd4F6 M3vob5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= M{DZeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NGTWW5RyUFSVIHHzd4F6 MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MnLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Myc / α-tubulin; 

PubMed: 25248858     


C. Effect of DFMO on c-Myc protein expression. A decrease in c-Myc expression was seen upon DFMO treatment.

25248858
Growth inhibition assay
2T1 cells; 

PubMed: 21093499     


AAT6 knockdown confers resistance to eflornithine. The RNAit program was used to design primers and the pRPaiSL construct was modified to target AAT6 for RNAi. The resulting hairpin RNAi constructs were transferred to 2T1 cells. For EC50 determination, cells were seeded at 2 × 103 ml−1 in 96-well plates in an eflornithine 2-fold dilution series. After 66 h growth, 20 μl of Alamar blue (AbD serotec) was added to each well and the plates incubated for a further 6 h. Fluorescence was determined using a Gemini Fluorescent Plate reader (Molecular Devices) at an excitation wavelength of 530 nm, an emission wavelength of 585 nm and a filter cut-off of 570 nm.

21093499
IHC
H&E staining of pancreas; 

PubMed: 25248858     


A. Histopathologic analysis of untreated and DFMO-treated pancreas using H&E staining. Pancreas from untreated animals showing poorly differentiated adenocarcinoma with some of the cells invading stroma (left panel). Pancreas from animals treated with DFMO showing PanIN lesions (right panels).

p21 / PCNA; 

PubMed: 25248858     


Effect of DFMO on pancreatic tumor cell proliferation. A. Immunohistochemical analysis for PCNA and p21 was performed on paraffin-embedded and micro-sectioned pancreatic tissues as described in the Methods section. A significantly decreased expression of PCNA and increased p21 expression was seen with DFMO treatment.

25248858
IHC/IF
ODC expression in pancreatic tumors; 

PubMed: 25248858     


Effect of DFMO on ODC expression in pancreatic tumors. Immunohistochemical and Immunofluorescence analyses were performed with paraffin-embedded and micro-sectioned pancreatic tissues as described in the Methods section. A significantly decreased expression of ODC was seen with DFMO treatment.

Cav-1 / β-catenin; 

PubMed: 25248858     


Effect of DFMO on cav-1 and β-catenin. Immunohistochemistry (top row of each set), Immunofluorescence (bottom row of each set) and mRNA analysis (bar graphs to the right) revealed a decrease in the cav-1 expression with both doses of DFMO; however, only the high dose (0.2%) caused a decrease in β-catenin expression.

25248858

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: BY2细胞
  • Concentrations: 2 mM
  • Incubation Time: 48 h
  • Method: 在BY2细胞中,加入或者不加入Difluoromethylornithine和cryptogein,观察这些化合物对细胞生长的影响和作用。
    (Only for Reference)

溶解度 (25°C)

体外 Water 47 mg/mL (198.61 mM)
DMSO Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 236.64
化学式

C6H12F2N2O2.HCl.H2O

CAS号 96020-91-6
储存条件 粉状
溶于溶剂
别名 Difluoromethylornithine hydrochloride hydrate, DFMO hydrochloride hydrate, RMI-71782 hydrochloride hydrate, α-difluoromethylornithine hydrochloride hydrate

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04696029 Recruiting Drug: Difluoromethylornithine Medulloblastoma Giselle SaulnierSholler|Atrium Health March 29 2021 Phase 2
NCT03536728 Recruiting Drug: AMXT1501|Drug: DFMO Cancer|Solid Tumor|Solid Carcinoma|Advanced Cancer Aminex Therapeutics Inc. June 12 2018 Phase 1
NCT02794428 Recruiting Drug: Eflornithine|Other: Eflornithine placebo Gastric Cancer|Gastric Intestinal Metaplasia Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI)|Cancer Prevention Pharmaceuticals Inc. September 19 2016 Phase 2
NCT02636569 Active not recruiting Drug: topical diclofenac daily|Drug: placebo Non-melanoma Skin Cancer University of Alabama at Birmingham February 2016 Not Applicable
NCT01636128 Withdrawn Drug: difluoromethylornithine|Drug: Sulindac Focus of Study: Drug Response Biomarkers Chemoprevention Neoplasms Cancer Prevention Pharmaceuticals Inc.|University of Arizona March 2014 Phase 2
NCT01586260 Active not recruiting Drug: DFMO Neuroblastoma Giselle SaulnierSholler|Cancer Prevention Pharmaceuticals Inc.|University of Arizona|University of Hawaii|University of Vermont|Beat NB Cancer Foundation|Atrium Health June 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID