エリブリン化学構造式

エリブリン

化学名:エリブリン

CAS番号.253128-41-5

英語名:Eribulin

CBNumberCB22546700

MFC40H59NO11

MW729.9

MOL File253128-41-5.mol

别名

(1S,4S,7S,10S,12R,14R,16S,18R,19R,20R,24R,27S,28S,29R,30S,31S,32R,33R)-6,13-ジメチレン-12-メチル-18-[(1S)-1-ヒドロキシ-2-アミノエチル]-19-メトキシ-17,35,36,37,38,39,40,41-オクタオキサノナシクロ[30.2.1.11,29.14,7.110,14.124,28.127,31.130,33.016,20]ヘンテトラコンタン-22-オン

エリブリン

(1S,5R,8S,9S,10S,11R,12R,13S,14R,16S,19S,22S,25S,27R,29R,31S,33R,34R)-33-[(2S)-3-アミノ-2-ヒドロキシプロピル]-34-メトキシ-27-メチル-21,28-ビス(メチレン)-5,9:8,12:10,16:11,14:13,16:19,22:25,29-ヘプタエポキシ-32-オキサビシクロ[29.3.0]テトラトリアコンタン-3-オン

エリブリン物理性質

比重(密度)	1.29±0.1 g/cm3(Predicted)
貯蔵温度	Store at -20°C
溶解性	Soluble in DMSO
外見	Powder
酸解離定数(Pka)	12.56±0.35(Predicted)
InChIKey	UFNVPOGXISZXJD-JBQZKEIOSA-N

危険有害性情報のコード(GHS)

エリブリン化学特性,用途語,生産方法

説明
The U.S. FDA approved eribulin mesylate (also referred to as E7389) in November 2010 for the treatment of metastatic breast cancer (MBC) for patients who previously received at least two chemotherapeutic regimens for late-stage disease. Eribulin is a synthetic analog of the marine natural product halichondrin B, which is isolated from the sea sponge Halichondria okadai. Eribulin retains most of the structural elements that constitute the right hand side of halichondrin B; structure–activity relationship (SAR) studies suggested that the antitumor activity of halichondrin B resides in that part of the molecule . Eribulin is a microtubule inhibitor that binds close to the vinca-binding site of tubulin. Unlike most tubulin inhibitors like taxanes, epothilones, and vinca alkaloids that inhibit microtubule dynamic instability by changing tubulin addition and loss parameters, eribulin’s effects on dynamic instability are novel in that eribulin inhibits the growth phase of microtubules without affecting the shortening phase by binding to microtubule plus ends.
使用
Eribulin is a anticancer drug and also is a fully synthetic macrocyclic ketone analogue of the marine natural product halichondrin B. It derived from a marine sponge (Lissodendoryx sp.) with antineoplastic activity.
定義
ChEBI: Eribulin is a fully synthetic macrocyclic ketone analogue of marine sponge natural products. Inhibits growth phase of microtubules via tubulin-based antimitotic mechanism, which leads to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage It has a role as an antineoplastic agent and a microtubule-destabilising agent. It is a macrocycle, a polyether, a polycyclic ether, a cyclic ketone, a primary amino compound and a cyclic ketal. It is a conjugate base of an eribulin(1+).
Mode of action
Eribulin is a non-taxane, microtubule dynamics inhibitor that increases survival of patients with metastatic breast cancer. Eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and, potentially, tumor regression.

エリブリン上流と下流の製品情報

エリブリン生産企業

253128-41-5, エリブリンキーワード

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エリブリン

危険有害性情報のコード(GHS)

エリブリン 化学特性,用途語,生産方法

エリブリン 上流と下流の製品情報

エリブリン 生産企業

253128-41-5, エリブリン キーワード

エリブリン化学特性,用途語,生産方法

エリブリン上流と下流の製品情報

エリブリン生産企業

253128-41-5, エリブリンキーワード