Formaat : 1mg
Synonyms: Maytansinoid DM1, DM1
| Description | Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM. |
| Targets & IC50 | CYP3A4:160.6 nM, CYP2C19:539.5 nM, UGT1A1:856.7 nM, CYP2C8:32.1 nM, UGT1A9:54.1 nM, CYP2B6:36.8 nM, CYP1A2:93.7 nM |
| In vitro | METHODS: HCT-15 and A431 cells were incubated with Mertansine (0-3 nM) for 72 hours, then the medium was removed from the plate and replaced with fresh medium. Allow the culture to grow and form colonies for 7-10 days after plating. Cultures were fixed, stained with 0.2% crystal violet in 10% formalin/PBS, and colonies were counted. RESULTS Mertansine can inhibit the growth of HCT-15 and A431 cells. [1] METHODS: 4T1 cells were incubated with Mertansine (5-100 μg/mL) for 4 hours, and cell viability was detected by CCk8. RESULTS Mertansine can inhibit the growth of 4T1 cells.[2] METHODS: MDA-MB-231 cells were incubated with Mertansine (0.001355–13.55μM) for 48 hours, and cancer cell viability was detected by MTT. RESULTS Mertansine can effectively inhibit the proliferation of MDA-MB-231 cells, with an IC50 value of 0.12 μM. [3] |
| In vivo | METHODS: The anti-tumor activity of Mertansine (0.5 mg/kg) was evaluated in mice with orthotopic 4T1 tumors. RESULTS Cancer cell apoptosis was significantly increased, and the effect was dose-dependent. [2] METHODS: The in vivo therapeutic properties of Mertansine were evaluated using MDA-MB-231 triple-negative breast tumor mice. Mertansine was administered every 3 days for a total of four injections at a dose of 0.8 mg/kg. RESULTS Mertansine demonstrated modest inhibition of cancer cell growth in MDA-MB-231 triple-negative mammary tumor mice.[3] |
| Synonyms | Maytansinoid DM1, DM1 |
| Molecular Weight | 738.29 |
| Formula | C35H48ClN3O10S |
| Cas No. | 139504-50-0 |
| Smiles | CO[C@@H]1\C=C/C=C(C)\Cc2cc(OC)c(Cl)c(c2)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCS)[C@@]2(C)O[C@H]2[C@H](C)[C@@H]2C[C@@]1(O)NC(=O)O2 |
| Relative Density. | 1.33 g/cm3 (Predicted) |
| Storage | Store at low temperature,The compound is unstable in solution. Please use soon, Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 83 mg/mL (112.42 mM), Sonication is recommended. The compound is unstable in solution. Please use soon.  H2O: < 0.1 mg/mL (insoluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (4.47 mM), Sonication is recommended.The compound is unstable in solution. Please use soon. 10% DMSO+90% Saline: < 10 mg/mL (13.54 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+ 5% Tween 80 + 45% Saline: 10 mg/mL (13.54 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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