에리불린

한글명:에리불린

카스 번호253128-41-5

상품명:Eribulin

CBNumberCB22546700

분자식C40H59NO11

포뮬러 무게729.9

MOL 파일253128-41-5.mol

동의어(한글)

에리불린

화학적 성질

밀도	1.29±0.1 g/cm3(Predicted)
저장 조건	Store at -20°C
용해도	DMSO에 용해됨
물리적 상태	가루
산도 계수 (pKa)	12.56±0.35(Predicted)
색상	White to off-white
InChIKey	UFNVPOGXISZXJD-JBQZKEIOSA-N

그림문자(GHS)

에리불린 화학적 특성, 용도, 생산

개요
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.
용도
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.
정의
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+).
부작용
Eribulin is an anti-cancer drug currently administered intravenously (IV) for the treatment of breast cancer and liposarcoma patients resistant to taxane therapy because of its excellent efficacy against taxane-resistant tumor types. Common side effects of Eribulin include: gastrointestinal reactions (dry mouth, nausea or vomiting, loss of appetite), weakness, pain, chills, cough, convulsions, frequent urination, nasal congestion, irregular heartbeat, difficulty breathing, decreased urine output, frequent urination, headache, etc. Other side effects include fainting, irregular heartbeat, repeated or severe allergic reactions, etc.
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.

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