エベロリムス

エベロリムス 価格 もっと(14)

メーカー	製品番号	製品説明	CAS番号	包装	価格	更新時間	購入
富士フイルム和光純薬株式会社(wako)	W01TRCE945400	Everolimus (〜90% pure)	159351-69-6	5mg	￥26100	2024-03-01	購入
富士フイルム和光純薬株式会社(wako)	W01TRCE945400	エベロリムス Everolimus	159351-69-6	10mg	￥34500	2024-03-01	購入
富士フイルム和光純薬株式会社(wako)	W01TOC6188	Everolimus	159351-69-6	10mg	￥60000	2024-03-01	購入
Sigma-Aldrich Japan	Y0002063	エベロリムス European Pharmacopoeia (EP) Reference Standard European Pharmacopoeia (EP) Reference Standard	159351-69-6	Y0002063	￥19100	2024-03-01	購入
Sigma-Aldrich Japan	Y0002061	システム適合性用エベロリムス European Pharmacopoeia (EP) Reference Standard European Pharmacopoeia (EP) Reference Standard	159351-69-6	Y0002061	￥77200	2024-03-01	購入

エベロリムス 化学特性,用途語,生産方法

外観

白色～うすい褐色、結晶性粉末～粉末

溶解性

エタノール及びアセトンに溶け、水にほとんど溶けない。

用途

細胞内 で FKBP12 と 複 合 体 を 形 成 し、mTOR（mammalian target of rapamycin）を選択的に阻害します。

用途

ラパマイシンの誘導体であり、 mTOR 阻害剤です。FK506 結合タンパク質 -12（FKBP-12）と結合して mTOR の活性を 阻害することにより、腫瘍細胞のシグナル伝 達を阻害し、腫瘍細胞の増殖を抑制する、ま た、腫瘍細胞からの VEGF の産生と VEGF に よる血管内皮細胞の増殖を抑制し、血管新生 を抑制すると考えられています。

効能

抗悪性腫瘍薬, 免疫抑制薬, mTOR阻害薬

商品名

アフィニトール (ノバルティスファーマ); アフィニトール (ノバルティスファーマ); サーティカン (ノバルティスファーマ)

説明

Everolimus, an oral immunosuppressant for the treatment of kidney and heart transplant rejection, is the 40-O-(2-hydroxyethyl) derivative of rapamycin. It has immunosuppressive properties similar to those of rapamycin, but with improved pharmacokinetic profile. Everolimus, like rapamycin, is a proliferation signal inhibitor that exerts its immunosuppressive effect by inhibiting the activation of p70 S6 kinase, thereby blocking growth factor-driven proliferation of T cells, B cells and vascular smooth muscle cells, and arresting cell cycle at the G1 phase. Inhibition of p70 S6 kinase activation by everolimus and rapamycin is mediated by their binding to FKBP12 (FK506 binding-protein 12). Everolimus inhibits FK506 binding to FKBP12 with an IC50 of 1.8–2.6 nM, and it is about 3- to 5-fold less potent than rapamycin (IC50=0.4–0.9 nM). The in vitro immunosuppressive activity of everolimus is also slightly less than that of rapamycin as demonstrated in a mixed lymphocyte reaction (MLR) assay (IC50=0.2–1.6 nM versus 0.07–0.5 nM, respectively) and in antigen-specific human helper T-cell clones (IC50=0.05–0.17nM versus 0.014–0.37nM, respectively). However, the in vivo immunosuppressive activity of oral everolimus 1–5 mg/ kg/day is similar to that of rapamycin at equivalent doses in rat models of renal or cardiac transplantation, localized graft-versus-host disease, and autoimmune glomerulonephritis. The recommended dosage of everolimus is 0.75 mg twice daily, and it is used in combination with cyclosporine microemulsion and corticosteroids.

化学的特性

Off White Solid

使用

Everolimus (IX) (SDZ-RAD), was developed by Novartis as an immunosuppressant to be used in conjunction with cyclosporin in transplantation allograft rejection and was recently approved in the US in 2003. Another natural product that had been approved for use in transplantation is rapamycin (sirolimus) as an inejectable agent. In an attempt to develop an orally bioavailable immunosuppressant agent, many companies attempted modification of rapamycin itself.

定義

ChEBI: Everolimus is a macrocyclic lactone that is rapamycin in which the hydroxy group attached to the cyclohexyl moiety has been converted into the corresponding 2-hydroxyethyl ether. It is an immunosuppressant and antineoplastic agent. It has a role as an antineoplastic agent, an immunosuppressive agent, a mTOR inhibitor, an anticoronaviral agent and a geroprotector. It is a primary alcohol, a secondary alcohol, an ether, a cyclic ketone, a cyclic acetal and a macrolide lactam. It is functionally related to a member of sirolimus.

一般的な説明

Everolimus, sold under trade names including Zortress^?, Certican, and Afinitor^?, is an immunosuppressant drug used to prevent rejection of organ transplants and to treat renal cell cancer and other tumors. This Certified Spiking Solution^? is suitable as starting material for calibrators, controls, or linearity standards for therapeutic drug monitoring or clinical and diagnostic testing of everolimus in patient whole blood samples by LC-MS/MS.

エベロリムス 上流と下流の製品情報

原材料

準備製品

エベロリムス 生産企業

名前	電話番号	電子メール	国籍	製品カタログ	優位度
AFINE CHEMICALS LIMITED	+86-0571-85134551	sales@afinechem.com	China	15414	58
Seasons Biotechnology Co., Ltd.	+86-0576-89232655 +86-13566878689	info@seasonsbio.com	China	47	58
BOC Sciences	16314854226; +16314854226	inquiry@bocsci.com	United States	19654	58
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	deasea125996@gmail.com	China	2472	58
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	997	58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.	+86-18600796368 +86-18600796368	sales@sjar-tech.com	China	485	58
Capot Chemical Co.,Ltd.	+86-（0）57185586718 +86-13336195806	sales@capot.com	China	29730	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1803	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21628	55
Shanghai Yingrui Biopharma Co., Ltd.	+86-21-33585366 - 03@	sales03@shyrchem.com	CHINA	738	60

159351-69-6(エベロリムス)キーワード:

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• 159351-69-6
• Everolimus（mixture of isomers）
• Everolimus powder
• CERTICAN; ZORTRESS; AFINITOR
• Rapamycin, 42-O-(2-hydroxyethyl)-
• Everolimus
• Certican
• CERTICAN(R)
• EveroliMus(RAD-001)
• (1R,9S,12S,15R,16Z,18R,19R,21R,23S,24Z,26Z,28Z,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-Methoxycyclohexyl]propan-2-yl]-19,30-diMethoxy-15,17,21,23,29,35-hexaMethyl-11,36-dioxa-4-azatricyclo[30.3.1.0^{4,9}]hexatriaconta-16,2
• Afinitor
• Zortress
• EveroliMus API
• Everolimus 159351-69-6
• 40-O-(2-Hydroxyethyl) Rapamycin
• EVEROLIMUS(2.0% BHT)
• EVEROLIMUS(WITHOUT BHT)
• 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine, rapamycin deriv
• Everolimus solution
• Everolimus, >=98%
• 42-O-(2-Hydroxyethyl)-rapamycin
• Certica
• RAD-001
• SDZRAD
• Everolimus (~90% pure)
• Everolimus USP/EP/BP
• Everolimus AFINITOR
• Everolimus (RAD-001, SDZ-RAD)
• MF No.: 230MF10023
• US-DMF ready
• US-DMF No.: 032020
• エベロリムス(異性体混合物)
• エベロリムス 溶液
• エベロリムス
• エベロリムス (JAN)
• (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-ジヒドロキシ-12-[(2R)-1-[(1S,3R,4R)-4-(2-ヒドロキシエトキシ)-3-メトキシシクロヘキシル]プロパン-2-イル]-19,30-ジメトキシ-15,17,21,23,29,35-ヘキサメチル-11,36-ジオキサ-4-アザトリシクロ[30.3.1.04,9]ヘキサトリアコンタ-16,24,26,28-テトラエン-2,3,10,14,20-ペンタオン
• (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-ジヒドロキシ-12-[(1R)-2-[(1S,3R,4R)-4-(2-ヒドロキシエトキシ)-3-メトキシシクロヘキシル]-1-メチルエチル]-19,30-ジメトキシ-15,17,21,23,29,35-ヘキサメチル-11,36-ジオキサ-4-アザトリシクロ[30.3.1.04,9]ヘキサトリアコンタン-16,24,26,28-テトラエン-2,3,10,14,20-ペンタオン
• アフィニトール
• エバロリムス
• 42-デオキシ-42-(2-ヒドロキシエトキシ)ラパマイシン
• (3S,7R,8R,11S,13S,14E,16E,18E,20S,22R,24R,25R,26E,28R,31S)-3,4-(テトラメチレン)-7,25-ジヒドロキシ-7,11-エポキシ-8,14,20,22,26,28-ヘキサメチル-13,24-ジメトキシ-31-[(1R)-1-メチル-2-[3β-メトキシ-4α-(2-ヒドロキシエトキシ)シクロヘキサン-1β-イル]エチル]-1-オキサ-4-アザ-14,16,18,26-シクロヘントリアコンタテトラエン-2,5,6,23,29-ペンタオン
• 42-O-(2-ヒドロキシエチル)ラパマイシン
• サーティカン