시롤리무스

시롤리무스 속성

시롤리무스 MSDS

Sirolimus

시롤리무스 C화학적 특성, 용도, 생산

화학적 성질

White to Off-White Solid

출처

Rapamycin was first discovered in 1972 in the soil of Easter Island produced by a bacterium called Streptomyces hygroscopicus. It takes its name from Rapa Nui, the indigenous name for the island. It is known clinically as sirolimus or Rapamune.

용도

Labelled Rapamycin. A triene macrolide antibiotic isolated from Streptomyces hygroscopicus. Name derived from the native word for Easter Island, Rapa?Nui. Used as an immunosuppressant; antirestenotic. This compound contains aproximately 2% d0.;Labeled Sir

Indications

Mechanistic target of rapamycin (mTOR) is a serine/threonine-specific protein kinase in the PI3/PI4-kinase family. mTOR was named after the natural macrolide rapamycin, also known as sirolimus, which was isolated from a soil sample from Easter Island in the 1970s and later evaluated as an immunosuppressive agent. The anticancer activity of rapamycin was discovered in the 1980s, although the mechanismof action and the identification of the rapamycin target, mTOR, were not elucidated until the 1990s. Rapamycin and its macrocyclic analogues, such as temsirolimus (Torisel(R), Wyeth/Pfizer) and everolimus (Afinitor(R), Novartis), are grouped as “rapalogs” that constitute the first-generation mTOR inhibitors.
Rapamycin was approved by the US FDA in 1999 as an immunosuppressive agent to prevent organ rejection in patients receiving kidney transplants. Although a large number of clinical studies have been performed to evaluate the anticancer activities of sirolimus in different types of cancers, such as invasive bladder cancer, breast cancer, and leukemia, most studies show limited efficacy. Outside oncological indications, sirolimus was approved by FDA for the treatment of a rare progressive lung disease lymphangioleiomyomatosis in 2015. Temsirolimus was approved for the treatment of advanced RCC. Everolimus was approved in the EU for the prevention of organ rejection in heart and kidney transplant recipients before FDA approved it in 2009 for the treatment of advanced RCC resistant to sunitinib or sorafenib and for the treatment of advanced or metastatic gastrointestinal and lung tumors in 2016. Additionally, rapamycin and rapalogs are being investigated as antiaging therapeutics or for the treatment of age-related diseases. Studies have revealed that mTOR activity can be retained under hypoxic conditions via mutations in the PI3K pathway, leading to increased translation and hypoxic gene expression and tumor progression.

정의

ChEBI: A macrolide isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.

일반 설명

Rapamycin is an anti-fungal antibiotic isolated from Streptomyces hygroscopicus. This antibiotic is active against all strains of Candida albicans. It blocks the signal transduction pathways required for the activation of T-helper cells.

생물학적 활성

Antifungal and immunosuppressant. Specific inhibitor of mTOR (mammalian target of Rapamycin). Complexes with FKBP-12 and binds mTOR inhibiting its activity. Inhibits interleukin-2-induced phosphorylation and activation of p70 S6 kinase.

시롤리무스 준비 용품 및 원자재

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시롤리무스 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Shanghai Minbiotech Co., Ltd.	+8617315815539	sales@minbiotech.com	CHINA	129	58
Hangzhou Benoy Chemical Co., Ltd	+8617342059697	sales@benoychem.com	China	315	58
Hebei Lingding Biotechnology Co., Ltd.	+86-18031140164 +86-19933155420	erin@hbldbiotech.com	China	878	58
Seasons Biotechnology Co., Ltd.	+86-0576-89232655 +86-13566878689	info@seasonsbio.com	China	46	58
Guangzhou Tengyue Chemical Co., Ltd.	+86-86-18148706580 +8618826483838	evan@tyvovo.com	China	152	58
BOC Sciences	+16314854226	inquiry@bocsci.com	United States	19743	58
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12456	58
Henan Tengmao Chemical Technology Co. LTD	+8615238638457	salesvip2@hntmhg.com	China	415	58
Hangzhou ICH Biofarm Co., Ltd	+undefined8613073685410	sales@ichemie.com	China	985	58
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	1000	58

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