Mertansine
Based on 28 publication(s) in Google Scholar
Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.75%
- CAS 番号: 139504-50-0
- 分子式: C35H48ClN3O10S
- 分子量:738.29
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Mertansine
More- Nature. 2024 Apr;628(8007):416-423. [Abstract]
- ACS Nano. 2025 Jul 1;19(25):23001-23010. [Abstract]
- Nat Commun. 2025 Apr 2;16(1):3167. [Abstract]
- Sci Transl Med. 2021 Feb 3;13(579):eabb6282. [Abstract]
- Adv Sci (Weinh). 2023 Mar;10(9):e2206912. [Abstract]
- Biomaterials. 2023 Jan:292:121913. [Abstract]
- J Exp Clin Cancer Res. 2023 Aug 9;42(1):200. [Abstract]
- J Control Release. 2024 Sep 5:375:74-89. [Abstract]
- J Control Release. 2024 Sep 19:375:438-453. [Abstract]
- J Control Release. 2021 Sep 10:337:431-447. [Abstract]
- Cell Rep Med. 2025 Sep 19:102365. [Abstract]
- BMC Med. 2022 Aug 24;20(1):257 [Abstract]
- Curr Biol. 2019 Jul 22;29(14):2259-2269.e4. [Abstract]
- Biomacromolecules. 2023 Feb 13;24(2):849-857. [Abstract]
- J Drug Deliv Sci Technol. 9 September 2022, 103770.
- Microb Cell Fact. 2021 Mar 10;20(1):67. [Abstract]
- iScience. 2025 May 7;28(6):112599. [Abstract]
- Sci Rep. 2020 Jun 1;10(1):8869. [Abstract]
- ACS Chem Biol. 2018 Mar 16;13(3):761-771. [Abstract]
- Curr Issues Mol Biol. 2023 Oct 5;45(10):8112-8125. [Abstract]
- Breast Cancer. 2022 Nov;29(6):1121-1132. [Abstract]
- Anticancer Res. 2020 Aug;40(8):4471-4479. [Abstract]
- STAR Protoc. 2022 Dec 16;3(4):101921. [Abstract]
- chemRxiv. 2026 May 3.
- bioRxiv. 2026 Jan 13:2026.01.12.699160. [Abstract]
- Patent. US20260000782A1.
- Patent. US20250228951A1.
- bioRxiv. 2023 Feb 14.
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Flow Cytometry
-
Cell Proliferation/Viability Assay
-
Cell Proliferation/Viability Assay
-
IF
ADC Payloads アイソフォーム固有の製品をすべて表示
More
生物活性
|
Maytansinoids |
Mertansine is a strong antiproliferative chemotherapeutics toward over 60 types of cancer cell lines[3].
Mertansine (0-1 μg/mL) shows antitumor activity in malignant B16F10 melanoma cells, and inhibits tumor cell growth by inhibiting mitosis when combined with DTX[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Malignant B16F10 melanoma cells[3]
-
Concentration:0, 0.01, 0.1, and 1 μg/mL
-
Incubation Time:4 h
-
Result:Showed antitumor activity in malignant B16F10 melanoma cells, with an IC50 of 0.092 μg/mL. Co-delivery of DTX and DM1, both of which inhibit tumor cell growth by inhibiting mitosis, is an effective strategy to achieve a combinatorial anticancer effect.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 139504-50-0
-
性状 Solid
-
分子量 738.29
-
分子式 C35H48ClN3O10S
-
Color White to light yellow
-
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
-
別名
DM1; Maytansinoid DM1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (28)
-
Journal Impact Factor
-
Most Recent
-
Nature
2024 Apr;628(8007):416-423. PMID: 38538786 -
ACS Nano
2025 Jul 1;19(25):23001-23010. PMID: 40522898 -
Nat Commun
Effective extracellular payload release and immunomodulatory interactions govern the therapeutic effect of trastuzumab deruxtecan (T-DXd). [Abstract]2025 Apr 2;16(1):3167. PMID: 40175391
Mertansine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 2;16(1):3167. [Abstract]
Various indicated cancer lines were seeded at low density and treated with titrated doses of DXd or DM1 (Mertansine, 0.1-10000 nM), with DMSO solvent used as control treatment group. Cells were cultured for 5 days or until control groups reached >90% confluency. Cell viability and drug induced toxicity were assessed by cellular ATP quantification using using CellTiter-Glo Luminescent Cell Viability Assay following manufacturer’s protocol. Nonlinear regression curve fit analysis were used to calculate IC50 values (n = 3 per group).
Mertansine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 2;16(1):3167. [Abstract]
Flow cytometry assessment of surface CD47 expression on Au565 cells after 2 days of treatment with DXd (Deruxtecan, 10-250 nM) or DM1 (Mertansine, 10-250 nM).
-
Sci Transl Med
Targeting tumor lineage plasticity in hepatocellular carcinoma using an anti-CLDN6 antibody-drug conjugate. [Abstract]2021 Feb 3;13(579):eabb6282. PMID: 33536280 -
Adv Sci (Weinh)
Overcoming the On-Target Toxicity in Antibody-Mediated Therapies via an Indirect Active Targeting Strategy. [Abstract]2023 Mar;10(9):e2206912. PMID: 36683161 -
Biomaterials
Disease-driven engineering of peptide-targeted DM1 loaded liposomal nanoparticles for enhanced efficacy in treating multiple myeloma by exploring DM1 prodrug chemistry. [Abstract]2023 Jan:292:121913. PMID: 36442437
Mertansine purchased from MedChemExpress. Usage Cited in: Biomaterials. 2023 Jan:292:121913. [Abstract]
Free Mertansine (DM1; 20 nM; 24 h) is able to induce apoptosis in NCI-H929 cells.
-
J Exp Clin Cancer Res
An amino acid transporter subunit as an antibody-drug conjugate target in colorectal cancer. [Abstract]2023 Aug 9;42(1):200. PMID: 37559159
Mertansine purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Aug 9;42(1):200. [Abstract]
HT29 and HCT116 cells were treated with the doses indicated of anti-CD98hc, anti-CD98hc-DM1 or Mertansine (DM1, 0.1-10 nM) for four days. The data are plotted as the percentage of MTT metabolization with respect to control.
-
J Control Release
2024 Sep 5:375:74-89. PMID: 39216599 -
J Control Release
Combination non-targeted and sGRP78-targeted nanoparticle drug delivery outperforms either component to treat metastatic ovarian cancer. [Abstract]2024 Sep 19:375:438-453. PMID: 39271060
Mertansine purchased from MedChemExpress. Usage Cited in: J Control Release. 2024 Sep 19:375:438-453. [Abstract]
Cytotoxicity of DM1 (Mertansine, 50-1000 nM) against OVCAR5, OVCAR8, and ID8 Trp53−/− ovarian cancer cell lines was determined at 72 h (left). Standard-of-care chemotherapeutics Paclitaxel (center) and Doxorubicin (right) showed similar order-of-magnitude IC50, compared to DM1, at 72 h. (IC50DM1 ≈ 50 nM, IC50Paclitaxel ≈ 10 nM (on OVCAR5 & OVCAR8), IC50paclitaxel ≈ 500 nM (on ID8 Trp53−/−), and IC50Doxorubicin ≈ 50 nM)
-
J Control Release
Polyethylene glycol-based linkers as hydrophilicity reservoir for antibody-drug conjugates. [Abstract]2021 Sep 10:337:431-447. PMID: 34329685 -
Cell Rep Med
FLT3L-based drug conjugate effectively targets chemoresistant leukemia stem cells in acute myeloid leukemia. [Abstract]2025 Sep 19:102365. PMID: 40975063 -
BMC Med
2022 Aug 24;20(1):257 PMID: 35999600 -
Curr Biol
Kinesin-5 Promotes Microtubule Nucleation and Assembly by Stabilizing a Lattice-Competent Conformation of Tubulin. [Abstract]2019 Jul 22;29(14):2259-2269.e4. PMID: 31280993 -
Biomacromolecules
2023 Feb 13;24(2):849-857. PMID: 36639133 -
-
Microb Cell Fact
Expression of a recombinant FLT3 ligand and its emtansine conjugate as a therapeutic candidate against acute myeloid leukemia cells with FLT3 expression. [Abstract]2021 Mar 10;20(1):67. PMID: 33691697 -
iScience
2025 May 7;28(6):112599. PMID: 40496813 -
Sci Rep
Rapid conjugation of antibodies to toxins to select candidates for the development of anticancer Antibody-Drug Conjugates (ADCs). [Abstract]2020 Jun 1;10(1):8869. PMID: 32483228 -
ACS Chem Biol
Toward a Microparticle-Based System for Pooled Assays of Small Molecules in Cellular Contexts. [Abstract]2018 Mar 16;13(3):761-771. PMID: 29365249 -
Curr Issues Mol Biol
Targeting GD2-Positive Tumor Cells by Pegylated scFv Fragment-Drug Conjugates Carrying Maytansinoids DM1 and DM4. [Abstract]2023 Oct 5;45(10):8112-8125. PMID: 37886955 -
Breast Cancer
A novel ADC targeting cell surface fibromodulin in a mouse model of triple-negative breast cancer. [Abstract]2022 Nov;29(6):1121-1132. PMID: 35982394 -
Anticancer Res
Novel Anti-CD70 Antibody Drug Conjugate for the Treatment of Adult T-Cell Leukemia (ATL). [Abstract]2020 Aug;40(8):4471-4479. PMID: 32727777 -
STAR Protoc
Identification and functional characterization of potential oncofetal targets in human hepatocellular carcinoma. [Abstract]2022 Dec 16;3(4):101921. PMID: 36595904 -
-
bioRxiv
A strategically designed homogeneous antibody-drug conjugate improves safety and therapeutic index in renal cell carcinoma. [Abstract]2026 Jan 13:2026.01.12.699160. PMID: 41648225 -
-
-
溶剤 & 溶解度
DMSO : 50 mg/mL (67.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.83 mg/mL (1.12 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.83 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (283 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Manu Lopus et al. Maytansine and Cellular Metabolites of Antibody-Maytansinoid Conjugates Strongly Suppress Microtubule Dynamics by Binding to Microtubules. [Content Brief]
[2]. Lopus M. Antibody-DM1 conjugates as cancer therapeutics. Cancer Lett. 2011 Aug 28;307(2):113-8. [Content Brief]
[3]. Zhong P, et al. cRGD-installed docetaxel-loaded mertansine prodrug micelles: redox-triggered ratiometric dual drug release and targeted synergistic treatment of B16F10 melanoma. Nanotechnology. 2017 Jul 21;28(29):295103. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3545 mL | 6.7724 mL | 13.5448 mL | 33.8620 mL |
| 5 mM | 0.2709 mL | 1.3545 mL | 2.7090 mL | 6.7724 mL | |
| 10 mM | 0.1354 mL | 0.6772 mL | 1.3545 mL | 3.3862 mL | |
| 15 mM | 0.0903 mL | 0.4515 mL | 0.9030 mL | 2.2575 mL | |
| 20 mM | 0.0677 mL | 0.3386 mL | 0.6772 mL | 1.6931 mL | |
| 25 mM | 0.0542 mL | 0.2709 mL | 0.5418 mL | 1.3545 mL | |
| 30 mM | 0.0451 mL | 0.2257 mL | 0.4515 mL | 1.1287 mL | |
| 40 mM | 0.0339 mL | 0.1693 mL | 0.3386 mL | 0.8466 mL | |
| 50 mM | 0.0271 mL | 0.1354 mL | 0.2709 mL | 0.6772 mL | |
| 60 mM | 0.0226 mL | 0.1129 mL | 0.2257 mL | 0.5644 mL |
Powered by Bioz