Imexon (BM 06002)
(Synonyms: 亚美克松; BM 06002) 目录号 : GC32952
Imexon (BM 06002) (BM 06002) 是一种具有抗癌活性的亚氨基吡咯烷酮氮丙啶。
Cas No.:59643-91-3
Sample solution is provided at 25 µL, 10mM.
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Imexon (BM 06002) is an iminopyrrolidone aziridine with anti-cancer activity.
Imexon (BM 06002) induces oxidative stress in the ER, activates an ER stress response. Imexon (BM 06002) does not significantly alter the levels of eIF2B5, however there is a dose-dependent increase in the phosphorylation of eIF2alpha, as well as an increase in the levels of GTP exchange protein eIF2B2 in MiaPaCa-2, Panc-1, and BxPC3 cells[1]. Imexon (BM 06002) induces single-stranded breaks in the human A375 melanoma cells but only significantly at the highest concentrations for each agent compared to controls. Imexon plus DTIC cytotoxicity is additive[2]. Imexon (BM 06002) show inhibitory activities against MiaPaCa-2, Panc-1 and BxPC3, with IC50s of 275.5 ± 54.2, 147.4 ± 4.7 and 355.7 ± 114.7 μM[3].
Imexon (BM 06002) in combination with DTIC results in an increase in the peak plasma imexon level in non-tumor-bearing mice. The combination of both drugs increases plasma imexon AUC by 22% (p=0.026). Imexon (BM 06002) (100 mg/kg/day, i.v.) treatment decreases the body weight of SCID mice bearing human A375 melanoma tumors, but there is no significant difference in tumor growth[2]. Imexon (BM 06002) (100 mg/kg) in combination with GEM shows synergistic inhibition of Panc-1 tumor growth in SCID mice.
[1]. Sheveleva EV, et al. Imexon induces an oxidative endoplasmic reticulum stress response in pancreatic cancer cells. Mol Cancer Res. 2012 Mar;10(3):392-400. [2]. Samulitis BK, et al. Interaction of dacarbazine and imexon, in vitro and in vivo, in human A375 melanoma cells. Anticancer Res. 2011 Sep;31(9):2781-5. [3]. Roman NO, et al. Imexon enhances gemcitabine cytotoxicity by inhibition of ribonucleotide reductase. Cancer Chemother Pharmacol. 2011 Jan;67(1):183-92.
Cell experiment: | Cell survival for the siRNA screening experiments are calculated by the conversion of resazurin to resorufin by metabolically active cells resulting in a fluorescent product. Confirmatory growth inhibition assays with eIF2b silencing are done using the methyl-thiazolyl-diphenyl-tetrazolium bromide (MTT) assay. Cell growth inhibition data are expressed as percent survival, compared to untreated cells. The IC50 is defined as the drug concentration required to produce 50% growth inhibition. |
Animal experiment: | The effect of the combination on tumor growth in vivo is evaluated in 25-30 g male SCID mice (n=8/group). Mice receive 5×106 A375 cells subcutaneously and are pair matched on day 30, when the average tumor burden is approximately 100 mm3. Treatment begins the following day, as follows: (i) saline vehicle control; (ii) 80 mg/kg/day DTIC; (iii) 100 mg/kg/day imexon; (iv) a combination of both drugs at the same doses. Drugs are administered (i.p.) for nine consecutive days and imexon is administered 15 min before DTIC when combined. Measurement of tumor burden and body weights are made every 3-4 days. Tumor burden (mm3) is calculated as (length × width2)/2. |
References: [1]. Sheveleva EV, et al. Imexon induces an oxidative endoplasmic reticulum stress response in pancreatic cancer cells. Mol Cancer Res. 2012 Mar;10(3):392-400. | |
| Cas No. | 59643-91-3 | SDF | |
| 别名 | 亚美克松; BM 06002 | ||
| Canonical SMILES | O=C1N2CC2C(N)=N1 | ||
| 分子式 | C4H5N3O | 分子量 | 111.1 |
| 溶解度 | Soluble in DMSO | 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 | 9.0009 mL | 45.0045 mL | 90.009 mL |
| 5 mM | 1.8002 mL | 9.0009 mL | 18.0018 mL |
| 10 mM | 0.9001 mL | 4.5005 mL | 9.0009 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。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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