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Purity: = 98.45%
Mertansine refers to the thiol-containing maytansinoid, DM1 (N2’-deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine) attached to a monoclonal antibody through reaction of the thiol group with an SPP (N-succinimidyl 4-(2-pyridyldithio)) linker to create an antibody-drug conjugate or ADC. Experimental ADCs with the SPP-DM1 design include lorvotuzumab mertansine. DM1 can also be linked to an antibody using the SMCC (4-(3-mercapto-2,5-dioxo-1-pyrrolidinylmethyl)-cylohexanecarboxylic acid) linker, in which case the International Nonproprietary Name of the conjugate formed contains the word emtansine. DM1 and its attachment via these linkers result from ImmunoGen Inc research. Trastuzumab emtansine (T-DM1) is an anti-HER2/neu antibody-drug conjugate.
| Targets |
Maytansinoids
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|---|---|
| ln Vitro |
When applied to more than 60 different types of cancer cell lines, mertansine is a potent antiproliferative chemotherapy[3].
Mertansine (0–1 μg/mL) has antitumor activity in malignant B16F10 melanoma cells and, when combined with DTX, inhibits tumor cell growth by blocking mitosis[3]. |
| ln Vivo |
The minimal maximum tolerated dose (MTD) of mertansine (DM1) is 1 mg/kg[3].
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| Cell Assay |
Cell Line: Malignant B16F10 melanoma cells[3]
Concentration: 0, 0.01, 0.1, and 1 μg/mL Incubation Time: 4 h Result: demonstrated antitumor activity, with an IC50 of 0.092 μg/mL, in malignant B16F10 melanoma cells. To achieve a combinatorial anticancer effect, co-delivering DTX and DM1, which both inhibit tumor cell growth by inhibiting mitosis, is a useful tactic. |
| References |
[2]. Lopus M. Antibody-DM1 conjugates as cancer therapeutics. Cancer Lett. 2011 Aug 28;307(2):113-8. [4].Koniev O, Kolodych S, Baatarkhuu Z, Stojko J, Eberova J, Bonnefoy JY, Cianférani S, Van Dorsselaer A, Wagner A. MAPN: First-in-Class Reagent for Kinetically Resolved Thiol-to-Thiol Conjugation. Bioconjug Chem. 2015 Sep 3. [Epub ahead of print] PubMed PMID: 26335849. |
| Molecular Formula |
C35H48CLN3O10S
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|---|---|
| Molecular Weight |
738.29
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| Exact Mass |
737.27
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| Elemental Analysis |
C, 56.94; H, 6.55; Cl, 4.80; N, 5.69; O, 21.67; S, 4.34
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| CAS # |
139504-50-0
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| Related CAS # |
139504-50-0;
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| Appearance |
White to off-white solid powder
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| SMILES |
C[C@@H]1[C@@H]2C[C@]([C@@H](/C=C\C=C(\CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)C[C@H]([C@]4(C1O4)C)OC(=O)[C@H](C)N(C)C(=O)CCS)C)/C)OC)(NC(=O)O2)O
|
| InChi Key |
ANZJBCHSOXCCRQ-GCRZMMRQSA-N
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| InChi Code |
InChI=1S/C35H48ClN3O10S/c1-19-10-9-11-26(46-8)35(44)18-25(47-33(43)37-35)20(2)31-34(4,49-31)27(48-32(42)21(3)38(5)28(40)12-13-50)17-29(41)39(6)23-15-22(14-19)16-24(45-7)30(23)36/h9-11,15-16,20-21,25-27,31,44,50H,12-14,17-18H2,1-8H3,(H,37,43)/b11-9-,19-10+/t20-,21+,25+,26-,27-,31?,34+,35+/m1/s1
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| Chemical Name |
(14S,16S,33S,2R,4R,10E,12Z,14R)-86-chloro-14-hydroxy-85,14-dimethoxy-33,2,7,10-tetramethyl-12,6-dioxo-7-aza-1(6,4)-oxazinana-3(2,3)-oxirana-8(1,3)-benzenacyclotetradecaphane-10,12-dien-4-yl N-(3-mercaptopropanoyl)-N-methyl-L-alaninate
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| Synonyms |
DM1; DM-1; DM 1; DM1; Compound DM1; [Maytansinoid]; Maytansinoid DM 1; Maytansinoid DM1; Maytansinoid DM-1; UNII-DDZ29HGH0E; maytansine; Mertansine; emtansine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 50~62.5 mg/mL ( 67.72~84.66 mM )
Ethanol : 2 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.17 mg/mL (2.94 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3545 mL | 6.7724 mL | 13.5448 mL | |
| 5 mM | 0.2709 mL | 1.3545 mL | 2.7090 mL | |
| 10 mM | 0.1354 mL | 0.6772 mL | 1.3545 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01853748 | Active, not recruiting | Drug: Trastuzumab Paclitaxel Trastuzumab emtansine |
Breast Cancer | Dana-Farber Cancer Institute | May 2013 | Phase 2 |
| NCT06125834 | Recruiting | Drug: Trastuzumab Emtansine (T-DM1) |
Advanced Breast Cancer Trastuzumab Emtansine |
The First Affiliated Hospital with Nanjing Medical University | June 1, 2023 | Phase 2 |
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