美登素DM1|Mertansine|139504-50-0|MFCD28398157-范德生物科技公司

美登素DM1

美登素DM1
NMR and HPLC COA下载 MSDS下载
Names：
Mertansine
CAS号：
139504-50-0
MDL Number： MFCD28398157
MF(分子式)： C35H48ClN3O10S MW(分子量)： 738.29
EINECS:No data available Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

美登素DM1(139504-50-0,Mertansine)具有抗肿瘤活性和微管蛋白调节剂的作用。它是α-氨基酸酯，氨基甲酸酯，环氧化物，有机杂环四环化合物，有机氯化合物，硫醇和美登木素生物碱。美登素DM1衍生自美登素。美登素DM1是抗体-药物偶联物中的细胞毒性成分，通过巯基与SPP（N-琥珀酰亚胺基4-（2-吡啶基二硫代））接头或SMCC（4-（3-mercapto-2， 5-二氧代-1吡咯烷基甲基）-环己烷甲酸）接头以产生抗体-药物偶联物。

货品编码	规格	纯度	价格 (¥)	现价(¥)	库存描述	数量	总计 (¥)
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
HCC327179-2.5mg	2.5mg	97%	¥ 998.00	¥ 998.00	4-7周	- +	¥ 0.00

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中文别名	美登素DM1(139504-50-0,Mertansine),N2'-去乙酰基-N2'-(3-巯基-1-氧代丙基)美登素
英文别名	Mertansine,139504-50-0
CAS号	139504-50-0
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
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 Molecular Weight	C35H48ClN3O10S
分子量 Formula	738.29
闪点 FP	520.5±34.3 °C
熔点 Melting point	No data available
沸点 Boiling point	937.1±65.0 °C at 760 mmHg
Polarizability极化度	75.0±0.5 10-24cm3
密度 Density	1.3±0.1 g/cm3
蒸汽压 Vapor Pressure	0.0±0.3 mmHg at 25°C
溶解度Solubility	DMSO溶解度≥ 83.33 mg/mL(112.87 mM)H2O< 0.1 mg/mL(insoluble)
性状	白色至灰白色固体粉末
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 * 该产品在溶液状态不稳定,建议您现用现配,即刻使用。

美登素DM1(139504-50-0,Mertansine)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染

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.

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产品说明	美登素DM1(139504-50-0,Mertansine)具有抗肿瘤活性和微管蛋白调节剂的作用。
Introduction	Maytansine DM1 (139504-50-0,美登素DM1) has anti-tumor activity and tubulin modulator effect.
Application1	美登素DM1是一种细胞毒素，它被用作抗体-药物偶联物的细胞毒性成分。
Application2
Application3

美登素DM1是一种微管蛋白抑制剂，美登素DM1在微管的末端结合并抑制微管的动态性。美登素是一种抗体可缀合的美登木素生物碱，用于克服与美登素相关的全身毒性并增强肿瘤特异性递送。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

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.

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