Mertansine是一种强效微管靶向化合物，可抑制微管蛋白组装形成微管，KD值为0.86µM。
Cas No.:139504-50-0
Sample solution is provided at 25 µL, 10mM.
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Mertansine is a potent microtubule-targeted compound that inhibits tubulin assembly into microtubules, with the KD value of 0.86µM [1]. Mertansine binds to the vinblastine-binding site in the mitochondrial region, leading to mitotic arrest and apoptosis-mediated cell death [2]. Mertansine has been extensively conjugated to antibodies via linkers containing disulfide bonds for highly efficient killing of cancer cells[3].
In vitro, Mertansine treatment for 72 hours significantly inhibited the proliferation of MCF7 cells with an IC50 value of 0.71nM[4]. Treatment with 2.5µM Mertansine for 48h significantly reduced CYP1A2, CYP2B6, and CYP3A4 mRNA levels in human hepatocytes[5].
References:
[1] Lopus M, Oroudjev E, Wilson L, et al. Maytansine and cellular metabolites of antibody-maytansinoid conjugates strongly suppress microtubule dynamics by binding to microtubules[J]. Molecular cancer therapeutics, 2010, 9(10): 2689-2699.
[2] Martin-Aubert S, Avrillon K, Tournier N, et al. Successful repositioning of mertansine for improved chemotherapy by combining a polymer prodrug approach and PET imaging[J]. Journal of Controlled Release, 2025, 378: 803-813.
[3] Lopus M. Antibody-DM1 conjugates as cancer therapeutics[J]. Cancer letters, 2011, 307(2): 113-118.
[4] Oroudjev E, Lopus M, Wilson L, et al. Maytansinoid-antibody conjugates induce mitotic arrest by suppressing microtubule dynamic instability[J]. Molecular cancer therapeutics, 2010, 9(10): 2700-2713.
[5] Choi W G, Park R, Kim D K, et al. Mertansine Inhibits mRNA Expression and Enzyme Activities of Cytochrome P450s and Uridine 5′-Diphospho-Glucuronosyltransferases in Human Hepatocytes and Liver Microsomes[J]. Pharmaceutics, 2020, 12(3): 220.
Mertansine是一种强效微管靶向化合物，可抑制微管蛋白组装形成微管，KD值为0.86µM[1]。Mertansine结合于线粒体区域的长春花碱结合位点，导致有丝分裂停滞及凋亡介导的细胞死亡[2]。Mertansine已广泛通过含二硫键的连接子与抗体偶联，以实现对癌细胞的高效杀伤[3]。
在体外，Mertansine处理72小时显著抑制了MCF7细胞的增殖，IC50值为0.71nM[4]。使用2.5µM的Mertansine处理人肝细胞48小时，显著降低了CYP1A2、CYP2B6和CYP3A4的mRNA水平[6]。
| Cell experiment [1]: | |
Cell lines | MCF7 cells |
Preparation Method | MCF7 cells were cultured as adherent cells in high glucose (4g/l) and 25mM HEPES-fortified DMEM supplemented with 1× nonessential amino acids and 10% fetal bovine serum (FBS) at 37°C in 5.8% CO2. Cells were plated onto a 96-well plate at a density of 2.4×104 cells/ml for 24h, and were treated with different concentrations of Mertansine (0.01, 0.1, 1, 10, 100, and 1000nM). After 72 hours, cell viability was analyzed. |
Reaction Conditions | 0.01, 0.1, 1, 10, 100, and 1000nM; 72h |
Applications | Mertansine treatment significantly reduced the cell viability of MCF7 cells in a dose-dependent manner. |
References: | |
| Cas No. | 139504-50-0 | SDF | |
| 别名 | 美登素,DM1; Maytansinoid DM1 | ||
| Canonical SMILES | C[C@]1([C@@](CC(N(C(C=C2C=C3OC)=C3Cl)C)=O)([H])OC([C@H](C)N(C)C(CCS)=O)=O)[C@H]([C@@H]([C@](OC4=O)([H])C[C@]([C@](/C=C/C=C(C)/C2)([H])OC)(N4)O)C)O1 | ||
| 分子式 | C35H48ClN3O10S | 分子量 | 738.29 |
| 溶解度 | DMSO : ≥ 83.33 mg/mL (112.87 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| 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 | 1.3545 mL | 6.7724 mL | 13.5448 mL |
| 5 mM | 270.9 μL | 1.3545 mL | 2.709 mL |
| 10 mM | 135.4 μL | 677.2 μL | 1.3545 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet