購物車 
-
美登素DM1
- names：
Mertansine
- CAS號：
139504-50-0
MDL Number： MFCD28398157 - MF(分子式)： C35H48ClN3O10S MW(分子量)： 738.29
- EINECS:No data available Reaxys Number:No data available
- Pubchem ID:11343137 Brand:BIOFOUNT
美登素DM1(139504-50-0,Mertansine)具有抗腫瘤活性和微管蛋白調節(jié)劑的作用。 它是α-氨基酸酯，氨基甲酸酯，環(huán)氧化物，有機雜環(huán)四環(huán)化合物，有機氯化合物，硫醇和美登木素生物堿。 美登素DM1衍生自美登素。美登素DM1是抗體-藥物偶聯(lián)物中的細胞毒性成分，通過巰基與SPP（N-琥珀酰亞胺基4-（2-吡啶基二硫代））接頭或SMCC（4-（3-mercapto-2， 5-二氧代-1吡咯烷基甲基）-環(huán)己烷甲酸）接頭以產生抗體-藥物偶聯(lián)物。
| 貨品編碼 | 規(guī)格 | 純度 | 價格 (￥) | 現(xiàn)價(￥) | 特價(￥) | 庫存描述 | 數(shù)量 | 總計 (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000900-5mg | 5mg | 98.7% | ￥ 890.00 | ￥ 890.00 | 2-3天 | ￥ 0.00 | ||
| YZM000900-2mg | 2mg | 98.7% | ￥ 536.00 | ￥ 536.00 | 2-3天 | ￥ 0.00 |
| 中文別名 | 美登素DM1(139504-50-0,Mertansine),N2'-去乙酰基-N2'-(3-巰基-1-氧代丙基)美登素 |
| 英文別名 | Mertansine,139504-50-0 |
| CAS號 | 139504-50-0 |
| Inchi | 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 |
| InchiKey | ANZJBCHSOXCCRQ-FKUXLPTCSA-N |
| 分子式 Formula | C35H48ClN3O10S |
| 分子量 Molecular Weight | 738.29 |
| 溶解度Solubility | Chloroform (Slightly, Sonicated), Methanol (Slightly) |
| 性狀 | 白色至灰白色固體粉末 |
| 儲藏條件 Storage conditions | -20°C 3 years年 4°C 2 years年 * 該產品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。 |
美登素DM1(139504-50-0,Mertansine)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質及有害物質產生，必要時實驗操作需要手套箱內完成以免對實驗人員造成傷害
3.實驗后產生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染
美登素DM1(139504-50-0,Mertansine) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
Tag:美登素DM1(139504-50-0,Mertansine),美登素DM1試劑,美登素DM1抑制劑,美登素DM1的作用,美登素DM1的純度,美登素DM1的使用,美登素DM1的合成,美登素DM1的外觀,美登素DM1的MSDS,美登素DM1的含量,美登素DM1的生產
| 產品說明 | 美登素DM1(139504-50-0,Mertansine)具有抗腫瘤活性和微管蛋白調節(jié)劑的作用。 |
| Introduction | Maytansine DM1 (139504-50-0,美登素DM1) has anti-tumor activity and tubulin modulator effect. |
| Application1 | 美登素DM1是一種細胞毒素，它被用作抗體-藥物偶聯(lián)物的細胞毒性成分。 |
| Application2 | |
| Application3 |
美登素DM1是一種微管蛋白抑制劑，美登素DM1在微管的末端結合并抑制微管的動態(tài)性。美登素是一種抗體可綴合的美登木素生物堿，用于克服與美登素相關的全身毒性并增強腫瘤特異性遞送。
| 警示圖 | |
| 危險性 | warning |
| 危險性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害 |
| 安全防護 | P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理 |
| 備注 | 實驗過程中防止吸入、食入，做好安全防護 |
| Preclinical safety profile of trastuzumab emtansine (T-DM1): mechanism of action of its cytotoxic component retained with improved tolerability |
| A phase II study of trastuzumab emtansine in patients with human epidermal growth factor receptor 2-positive metastatic breast cancer who were previously treated with trastuzumab, lapatinib, an anthra |
| Drug interaction potential of trastuzumab emtansine (T-DM1) combined with pertuzumab in patients with HER2-positive metastatic breast cancer |
| Phase I multidose-escalation study of the anti-CD19 maytansinoid immunoconjugate SAR3419 administered by intravenous infusion every 3 weeks to patients with relapsed/refractory B-cell lymphoma |
| HER2 testing in patients with breast cancer |
1.Hyaluronic Acid-Shelled Disulfide-Cross-Linked Nanopolymersomes for Ultrahigh-Efficiency Reactive Encapsulation and CD44-Targeted Delivery of Mertansine Toxin.
Zhang Y;Wu K;Sun H;Zhang J;Yuan J;Zhong Z ACS Appl Mater Interfaces. 2018 Jan 17;10(2):1597-1604. doi: 10.1021/acsami.7b17718. Epub 2018 Jan 4.
It was and remains a big challenge for cancer nanomedicines to achieve high and stable drug loading with fast drug release in the target cells. Here, we report on novel hyaluronic acid-shelled disulfide-cross-linked biodegradable polymersomes (HA-XPS) self-assembled from hyaluronic acid-b-poly(trimethylene carbonate-co-dithiolane trimethylene carbonate) diblock copolymer for ultrahigh-efficiency reactive encapsulation and CD44-targeted delivery of mertansine (DM1) toxin, a highly potent warhead for clinically used antibody-drug conjugates. Remarkably, HA-XPS showed quantitative encapsulation of DM1 even with a high drug loading content of 16.7 wt %. DM1-loaded HA-XPS (HA-XPS-DM1) presented a small size of ∼80 nm, low drug leakage under physiological conditions, and fast glutathione-triggered drug release. MTT assays revealed that HA-XPS was noncytotoxic while HA-XPS-DM1 was highly potent to MDA-MB-231 cells with an IC;50; comparable to that of free DM1. The in vitro and in vivo inhibition experiments indicated that HA-XPS could actively target MDA-MB-231 cells. Notably, HA-XPS-DM1 while causing little adverse effect could effectively inhibit tumor growth and significantly prolong survival time in MDA-MB-231 human breast tumor-bearing mice.
Zhang Y;Wu K;Sun H;Zhang J;Yuan J;Zhong Z ACS Appl Mater Interfaces. 2018 Jan 17;10(2):1597-1604. doi: 10.1021/acsami.7b17718. Epub 2018 Jan 4.
It was and remains a big challenge for cancer nanomedicines to achieve high and stable drug loading with fast drug release in the target cells. Here, we report on novel hyaluronic acid-shelled disulfide-cross-linked biodegradable polymersomes (HA-XPS) self-assembled from hyaluronic acid-b-poly(trimethylene carbonate-co-dithiolane trimethylene carbonate) diblock copolymer for ultrahigh-efficiency reactive encapsulation and CD44-targeted delivery of mertansine (DM1) toxin, a highly potent warhead for clinically used antibody-drug conjugates. Remarkably, HA-XPS showed quantitative encapsulation of DM1 even with a high drug loading content of 16.7 wt %. DM1-loaded HA-XPS (HA-XPS-DM1) presented a small size of ∼80 nm, low drug leakage under physiological conditions, and fast glutathione-triggered drug release. MTT assays revealed that HA-XPS was noncytotoxic while HA-XPS-DM1 was highly potent to MDA-MB-231 cells with an IC;50; comparable to that of free DM1. The in vitro and in vivo inhibition experiments indicated that HA-XPS could actively target MDA-MB-231 cells. Notably, HA-XPS-DM1 while causing little adverse effect could effectively inhibit tumor growth and significantly prolong survival time in MDA-MB-231 human breast tumor-bearing mice.
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