169869-90-3|依喜替康甲磺酸盐|Exatecan Mesylate|MFCD04113012-范德生物科技公司

依喜替康甲磺酸盐

NMR下载 COA and HPLC MSDS下载
names：
Exatecan Mesylate
CAS号：
169869-90-3
MDL Number： MFCD04113012
MF(分子式)： C25H26FN3O7S MW(分子量)： 531.55
EINECS: Reaxys Number:
Pubchem ID:6918249 Brand:BIOFOUNT

依沙替康甲磺酸盐(169869-90-3,Exatecan Mesylate) 是一种有效的 DNA 拓扑异构酶 I (topoisomerase I) 的抑制剂，IC50值是 2.2 μM (0.975 μg/mL)，可用于癌症研究

货品编码	规格	纯度	价格 (¥)	现价(¥)	库存描述	数量	总计 (¥)
YZM002770-100mg	100mg	99%	¥ 0.00	¥ 0.00	2-3天	- +	¥ 0.00
YZM002770-10mg	10mg	99%	¥ 7980.00	¥ 7980.00	2-3天	- +	¥ 0.00
YZM002770-5mg	5mg	99%	¥ 4680.00	¥ 4680.00	2-3天	- +	¥ 0.00
YZM002770-1mg	1mg	99%	¥ 1580.00	¥ 1580.00	2-3天	- +	¥ 0.00

大包装询价提供各种包装，敬请垂询
收藏商品商品点评加入购物车立即购买

快速询价

收起

你想询价的产品

*产品名称：

CAS号：

产品编号：

需求描述：

请准确填写您的联系方式，以便为您提供最好的服务。

*公司名称：

*电子邮箱：

联系人：

*电话：

*验证码：

询价

中文别名	依喜替康甲磺酸盐;依沙替康甲磺酸盐(169869-90-3,Exatecan Mesylate);依喜替康甲磺酸盐
英文别名	Exatecan Mesylate(169869-90-3);Exatecan mesilate;Exatecan (Mesylate);DX 8951f;DX-8951f
CAS号	169869-90-3
SMILES	O=S(C)(O)=O.O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O
Inchi	InChI=1S/C24H22FN3O4.CH4O3S/c1-3-24(31)14-6-18-21-12(8-28(18)22(29)13(14)9-32-23(24)30)19-16(26)5-4-11-10(2)15(25)7-17(27-21)20(11)19;1-5(2,3)4/h6-7,16,31H,3-5,8-9,26H2,1-2H3;1H3,(H,2,3,4)/t16-,24-;/m0./s1
InchiKey	BICYDYDJHSBMFS-GRGFAMGGSA-N
分子式 Formula	C25H26FN3O7S
分子量 Molecular Weight	531.55
闪点 FP	No data available
熔点 Melting point	No data available
沸点 Boiling point	No data available
Polarizability极化度	No data available
密度 Density	No data available
蒸汽压 Vapor Pressure	No data available
溶解度Solubility	生物体外In Vitro:DMSO溶解度8.33 mg/mL(15.67 mM;Need ultrasonic)H2O : 6 mg/mL(11.29 mM;Need ultrasonic and warming)
性状	棕色到卡其色固体粉末
储藏条件 Storage conditions	4°C，在氮气下储存

依沙替康甲磺酸盐(169869-90-3,Exatecan Mesylate)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

Exatecan Mesylate(169869-90-3) 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:依沙替康甲磺酸盐(169869-90-3,Exatecan Mesylate),依沙替康甲磺酸盐试剂,依沙替康甲磺酸盐的纯度,依沙替康甲磺酸盐的厂家,依沙替康甲磺酸盐的价格,依沙替康甲磺酸盐的作用,依沙替康甲磺酸盐的外观,依沙替康甲磺酸盐的溶解度,依沙替康甲磺酸盐的MSDS

产品说明	依喜替康甲磺酸盐(169869-90-3,Exatecan Mesylate)是喜树碱的半合成水溶性衍生物，具有抗肿瘤活性。
Introduction	Exatecan mesylate (169869-90-3,依沙替康甲磺酸盐) is a semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity.
Application1	依沙替康甲磺酸盐可通过稳定拓扑异构酶I与DNA之间的可裂解复合物并抑制DNA断裂的连接来抑制拓扑异构酶I的活性，从而抑制DNA复制并触发凋亡性细胞死亡。
Application2	依沙替康甲磺酸盐不需要酶促活化，并且比喜树碱和其他喜树碱类似物具有更高的效力。
Application3

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

Key role of topoisomerase I inhibitors in the treatment of recurrent and refractory epithelial ovarian carcinoma(Expert review of anticancer therapy,2008)

Relationship between drug release of DE-310, macromolecular prodrug of DX-8951f, and cathepsins activity in several tumors(Biological & pharmaceutical bulletin,2007)

Does consolidation with autologous stem cell transplantation improve the outcome of children with metastatic or relapsed Ewing sarcoma?(Pediatric blood & cancer,2007)

Exatecan in pretreated adult patients with advanced soft tissue sarcoma: results of a phase II--study of the EORTC Soft Tissue and Bone Sarcoma Group

Quantitative acid hydrolysis of DE-310, a macromolecular carrier system for the camptothecin analog DX-8951f(Journal of pharmaceutical and biomedical analysis,2007)

1. A phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for 5 days every 3 weeks to patients with advanced ovarian, tubal or peritoneal cancer resistant to platinum, taxane and topotecan
Claire F. Verschraegen, Andrzej P. Kudelka, Wei Hu. Cancer Chemother Pharmacol (2004) 53: 1–7
Exatecan mesylate (DX-8951f) is a synthetic derivative of camptothecin, a natural alkaloid extracted from the bark and leaves of the tree, Camptotheca acuminata. The activity of the drug is linked to its lactone form, which is in equilibrium with a carboxylate (open E ring) form. The equilibrium favors the carboxylate form at physiologic pH. The chemical structure of exatecan mesylate (DX-8951f) has been modi?ed to render the molecule water soluble by adding a ring structure between rings A (in position 9) and B (in position 7), and a ?uor in position 11. DX-8951f has shown both high in vitro potency against a series of 32 malignant cell lines and signi?cant topoisomerase I inhibition. The antiproliferative activity of exatecan mesylate (DX-8951f) in this system was 28 times greater than that of topotecan, and the antiproliferative activity of DX-8951f was about seven times greater than that of SN-38 (an active metabolite of irinotecan). Because of the demonstration of greater activity of DX-8951f than other camptothecin derivatives at equimolar concentrations in these pre- clinical studies, this phase II study was initiated.

2. DE-310, a macromolecular prodrug of the topoisomerase-I-inhibitor exatecan (DX-8951), in patients with operable solid tumors
Moritz N. Wente1 ,Jorg Kleeff, Markus W. Buchler. Investigational New Drugs 23: 339–347, 2005.
One of the recently introduced members of camptothecin analogs, exatecan mesylate (DX-8951f), is a synthetic water-soluble hexacyclic camptothecin analogue with broad anti-tumor activity. In pre-clinical studies, DX-8951 revealed highly potent inhibition of tumor cell growth in vitro and in vivo,evenin cells resistant to other members of the camptothecin family. In com- parison to other camptothecins, DX-8951 showed up to 20-fold higher topoisomerase-I inhibition and up to 30-fold more potent cell growth inhibition in vitro in various cancer cell lines.With its anti-tumor activity against irinotecan- and topotecan-resistant tumors, in phase II clinical DX-8951 demonstrated anti-tumor activity in several cancer types; phase III studies in pancreatic cancerare ongoing.

3. A phase II clinical and pharmacokinetic study of intravenous exatecan mesylate (DX-8951f) in patients with untreated metastatic gastric cancer
Jaffer A. Ajani, Chris Takimoto, Carlos R. Becerra. Investigational New Drugs 23: 479–484, 2005
Exatecan mesylate (DX-8951f; Daiichi Pharmaceutical Co., Ltd., Japan) is a synthetic camptothecin analogue (Figure 1) that is amore potent inhibitor of topoisomerase I than camptothecin, topotecan, and the active metabolite of irinotecan, SN-38. In preclinical studies, DX-8951f demonstrated broad antitumor activity compared with available camptothecin analogues. Cyclical dosing at lower doses demonstrated higher antitumor activity compared to single dose administration. Furthermore, the antitumor activity documented in phase I trials made DX-8951f an attractive compound for clinical development. We have completed a phase II trial designed to evaluate the activity and toxicity of exatecan mesylate (DX-8951f) in patients with previously untreated gastric carcinoma given as a thirty minute infusion daily for 5 days every 3 weeks. This schedule was selected from six phase I regimens because of the level of antitumor activity observed and its favorable toxicity pro?le.

对不起，暂无产品评价！

MSDS

SDS 1.0 中文

展开

SDS 1.0 英文

展开