Piperazine Erastin
目录号 : GC36926
A ferroptosis inducer
Cas No.:1538593-71-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Piperazine erastin is an inducer of ferroptosis.1,2 It inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC50 = 0.8 ?M), indicating inhibition of the system xc- cystine/glutamate transporter, and decreases glutathione (GSH) levels in HT-1080 fibrosarcoma cells when used at a concentration of 10 ?M. Piperazine erastin inhibits the growth of BJeLR cells overexpressing the H-Ras activating mutation H-RasG12V (IC50 = 0.3 ?M).1 It increases hepatic mRNA expression of the gene encoding Cox-2 and prevents tumor formation in an HT-1080 mouse xenograft model when administered at a dose of 60 mg/kg.2
1.Larraufie, M.-H., Yang, W.S., Jiang, E., et al.Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubilityBioorg. Med. Chem. Lett.25(21)4787-4792(2015) 2.Yang, W.S., SriRamaratnam, R., Welsch, M.E., et al.Regulation of ferroptotic cancer cell death by GPX4Cell156(1-2)317-331(2014)
| Cas No. | 1538593-71-3 | SDF | |
| Canonical SMILES | O=C1N(C2=CC(CN3CCNCC3)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=C1C=CC=C6 | ||
| 分子式 | C35H41ClN6O4 | 分子量 | 645.19 |
| 溶解度 | DMSO: 33.33 mg/mL (51.66 mM); Water: < 0.1 mg/mL (insoluble) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5499 mL | 7.7497 mL | 15.4993 mL |
| 5 mM | 0.31 mL | 1.5499 mL | 3.0999 mL |
| 10 mM | 0.155 mL | 0.775 mL | 1.5499 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。
Transferrin Receptor Is a Specific Ferroptosis Marker
Cell Rep 2020 Mar 10;30(10):3411-3423.e7.PMID:32160546DOI:10.1016/j.celrep.2020.02.049.
Ferroptosis is a type of regulated cell death driven by the iron-dependent accumulation of oxidized polyunsaturated fatty acid-containing phospholipids. There is no reliable way to selectively stain ferroptotic cells in tissue sections to characterize the extent of ferroptosis in animal models or patient samples. We address this gap by immunizing mice with membranes from lymphoma cells treated with the ferroptosis inducer Piperazine Erastin and screening ∼4,750 of the resulting monoclonal antibodies generated for their ability to selectively detect cells undergoing ferroptosis. We find that one antibody, 3F3 ferroptotic membrane antibody (3F3-FMA), is effective as a selective ferroptosis-staining reagent. The antigen of 3F3-FMA is identified as the human transferrin receptor 1 protein (TfR1). We validate this finding with several additional anti-TfR1 antibodies and compare them to other potential ferroptosis-detecting reagents. We find that anti-TfR1 and anti-malondialdehyde adduct antibodies are effective at staining ferroptotic tumor cells in multiple cell culture and tissue contexts.