产品描述: | 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) |
靶点: |
Maytansinoids;MicrotubuleAssociated |
体外研究: |
Mertansine is a strong antiproliferative chemotherapeutics toward over 60 types of cancer cell lines. 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. Cell Proliferation Assay Cell Line: Malignant B16F10 melanoma cells 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. |
体内研究: |
Mertansine (DM1) has a low maximum-tolerated dose (MTD) of 1 mg/kg |
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. 2. Lopus M. Antibody-DM1 conjugates as cancer therapeutics. Cancer Lett. 2011 Aug 28;307(2):113-8. 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. |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.354 ml |
6.772 ml |
13.545 ml |
5 mM |
0.271 ml |
1.354 ml |
2.709 ml |
10 mM |
0.135 ml |
0.677 ml |
1.354 ml |
50 mM |
0.027 ml |
0.135 ml |
0.271 ml |
|
注意: |
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