Oxamflatin
(Synonyms: Metacept-3) 目录号 : GC17472
Inhibitor of histone deacetylases
Cas No.:151720-43-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cells grown in DMEM supplemented with 10% fetal bovine serum are challenged with serial two fold dilutions of oxamflatin on day 1 after the cells are seeded, and incubated for 2 days for the suspension cell cultures and for 3 days for the adherent cell cultures. Inhibition of the cell growth by oxamflatin is determined by staining with MTT as described previously[1]. |
Animal experiment: | Mice: Oxamflatin is injected intraperitoneally into BDF1 mice on day 1, 3, 5, 7, 9 and 11 and after the intraperitoneal inoculation of single cell suspension of the B16 melanoma cells. The survival days of the animals are recorded and the percent of increased life span (ILS%) is calculated[1]. |
References: [1]. Kim YB, et al. Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase. Oncogene. 1999 Apr 15;18(15):2461-70. | |
Oxamflatin is a potent histone deacetylase inhibitor with IC50 value of 15.7 nM [1].
Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription.
Oxamflatin is a potent histone deacetylase inhibitor and a novel antitumor compound. In mouse and human tumor cell lines, such as P388, Lewis, Lu-99, HT-29 and HeLa cells, Oxamflatin exhibited antiproliferative activity. In HeLa cells, Oxamflatin changed cell morphology, and significantly reduced the number of the cells in S phase and increased the number of cells in G0/G1 phase [1]. In the HIV-1 latently infected Jurkat T cell line, Oxam?atin increased the acetylation level of histone H3 and histone H4 at the nucleosome 1(nuc-1) site of the HIV-1 LTR and activated HIV-1 gene expression by 2-17 fold, suggesting that Oxam?atin has potential as drug candidates as antilatency therapies [2]. In OVCAR-5 and SKOV-3 ovarian cancer cell lines, oxamflatin decreased cell viability and significantly inhibited DNA synthesis and cell proliferation. Also, oxamflatin reduced the expression of c-Myc, CDK4 and E2F1, and the phosphorylation level of Rb protein, but upregulated p21 [3].
In mice transplanted with B16 murine melanoma, Oxamflatin (20 mg/kg) injected intraperitoneally six times on day 1, 3, 5, 7, 9 and 11 significantly increased the days of survival [1].
References:
[1].Kim YB, Lee KH, Sugita K, et al. Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase. Oncogene. 1999 Apr 15;18(15):2461-70.
[2].Yin H, Zhang Y, Zhou X, et al. Histonedeacetylase inhibitor Oxamflatin increase HIV-1 transcription by inducing histone modification in latently infected cells. Mol Biol Rep. 2011 Nov;38(8):5071-8.
[3].Wang YL, Liui HL, Fu RG, et al. HDAC Inhibitor Oxamflatin Induces Morphological Changes and has Strong Cytostatic Effects in Ovarian Cancer Cell Lines. Curr Mol Med. 2016;16(3):232-42.
| Cas No. | 151720-43-3 | SDF | |
| 别名 | Metacept-3 | ||
| 化学名 | (1Z,2E)-N-hydroxy-5-(3-(phenylsulfonamido)phenyl)pent-2-en-4-ynimidic acid | ||
| Canonical SMILES | OC(/C([H])=C([H])/C#CC1=CC(NS(C2=CC=CC=C2)(=O)=O)=CC=C1)=N\O | ||
| 分子式 | C17H14N2O4S | 分子量 | 342.37 |
| 溶解度 | DMF: 10 mg/ml,DMF:PBS (pH 7) (1:10): 0.1 mg/ml,DMSO: 5 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml,Ethanol: 0.5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9208 mL | 14.6041 mL | 29.2082 mL |
| 5 mM | 0.5842 mL | 2.9208 mL | 5.8416 mL |
| 10 mM | 0.2921 mL | 1.4604 mL | 2.9208 mL |
| 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 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。