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エベロリムス

エベロリムス 化学構造式
159351-69-6
  • CAS番号.159351-69-6
  • 化学名:エベロリムス
  • 别名: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)
  • 英語化学名:Everolimus
  • 英語别名:SDZRAD;Certica;RAD-001;Zortress;Afinitor;Certican;Everolimus;CERTICAN(R);EveroliMus API;Everolimus powder
  • CBNumber:CB9502411
  • Molecular Formula:C53H83NO14
  • Formula Weight:958.22
  • MOL File:159351-69-6.mol
エベロリムス 物理性質
  • 融点  :NA
  • 沸点  :998.7±75.0 °C(Predicted)
  • 比重(密度)  :1.18±0.1 g/cm3(Predicted)
  • 闪点  :2℃
  • 貯蔵温度  :-20°C
  • 酸解離定数(Pka) :10.40±0.70(Predicted)
  • 水溶解度  :Soluble in dimethysulfoxide,ethanol and chloroform. Slightly soluble in water.
  • 安定性: :Hygroscopic
  • InChIKey :HKVAMNSJSFKALM-GKUWKFKPSA-N
安全性情報
危険有害性情報のコード(GHS)
  • 絵表示(GHS)
  • 注意喚起語Danger
  • 危険有害性情報
  • H225:引火性の高い液体および蒸気
  • H319:強い眼刺激
  • H372:長期にわたる、または反復暴露により臓器の障 害
  • 注意書き
  • P210:熱/火花/裸火/高温のもののような着火源から遠ざ けること。-禁煙。
  • P260:粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。
  • P264:取扱い後は皮膚をよく洗うこと。
  • P264:取扱い後は手や顔をよく洗うこと。
  • P270:この製品を使用する時に、飲食または喫煙をしないこ と。
  • P305+P351+P338:眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。
  • P314:気分が悪い時は、医師の診断/手当てを受けること。
エベロリムス 価格 もっと(8)
  • メーカー: 富士フイルム和光純薬株式会社(wako)
  • 製品番号: W01TRCE945400
  • 製品説明 : 
  • 純度: Everolimus (〜90% pure)
  • 包装: 5mg
  • 価格: ¥13800
  • 更新時間: 2021/03/23
  • 購入: 購入
  • メーカー: 富士フイルム和光純薬株式会社(wako)
  • 製品番号: W01TRCE945400
  • 製品説明 : エベロリムス
  • 純度: Everolimus
  • 包装: 10mg
  • 価格: ¥18800
  • 更新時間: 2021/03/23
  • 購入: 購入
  • メーカー: 富士フイルム和光純薬株式会社(wako)
  • 製品番号: W01TOC6188
  • 製品説明 : 
  • 純度: Everolimus
  • 包装: 10mg
  • 価格: ¥47000
  • 更新時間: 2021/03/23
  • 購入: 購入
  • メーカー: Sigma-Aldrich Japan
  • 製品番号: E-068
  • 製品説明 : エベロリムス 溶液
  • 純度: Everolimus solution1.0?mg/mL in acetonitrile, ampule of 1?mL, certified reference material
  • 包装: 1ml
  • 価格: ¥63600
  • 更新時間: 2021/03/23
  • 購入: 購入
  • メーカー: 富士フイルム和光純薬株式会社(wako)
  • 製品番号: W01W0105-0914
  • 製品説明 : エベロリムス(異性体混合物)
  • 純度: Everolimus (mixture of isomers)97.0+%(HPLC)(異性体混合)
  • 包装: 25mg
  • 価格: ¥51800
  • 更新時間: 2021/03/23
  • 購入: 購入

Everolimus 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. In addition, the 40-O-(2-hydroxyethyl) group alters the physico-chemical properties of the macrolide to allow galenic formulation. Everolimus is prepared in a two-step semisynthesis starting from rapamycin, by alkylation of the 40-hydroxyl group with t-butyldimethylsilyloxyethyl triflate and subsequent cleavage of the silyl protecting group. 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. Following oral dosing, the peak concentration (Cmax) of everolimus is estimated between 1.5 to 2 hours, and steady state is achieved within 4 days. The terminal elimination half-life is 21 to 35 hours. By comparison, rapamycin has a longer elimination half-life (60 hours) and longer time to reach steady state (7 to 14 days). Consequently, rapamycin treatment requires a large loading dose, followed by once daily maintenance dose, whereas everolimus is administered twice daily but without the need of a loading dose. Everolimus is extensively metabolized, primarily by CYP3A4. Approximately 80% of the dose is excreted in the feces and about 5% in the urine. In clinical trials with adult cardiac transplant recipients, oral everolimus 0.75 or 1.5 mg twice daily significantly reduced the incidence of efficacy failure as well as cardiac allograft vasculopathy (CAV) up to 2 years after transplantation as compared with azathioprene 1–3 mg/kg/day. However, graft and patient survival rates at 1 year were similar in patients receiving everolimus and azathioprene. In trials involving renal transplant recipients, the combined incidence of biopsy-confirmed acute rejection, graft loss, death, or loss to follow-up was similar in patients receiving everolimus 1.5 or 3 mg/day or mycophenolate mofetil 2 g/day up to 3 years after transplantation. Everolimus was well tolerated in transplant patients. The incidence of viral infection including cytomegalovirus (CMV) was reduced in comparison to azathioprene and mycophenolate mofetil, but bacterial infections were more frequent. Main adverse events associated with everolimus were thrombocytopenia, leucopenia, and elevated serum lipids and creatinine.
  • 化学的特性 Off White Solid
  • Originator Novartis (Switzerland)
  • 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.
  • 使用 Macrolide immunosuppressant; derivative of Rapamycin. Inhibits cytokine-mediated lymphocyte proliferation
  • 使用 Everolimus Macrolide immunosuppressant; Everolimus is a derivative of Rapamycin. Everolimus inhibits cytokine-mediated lymphocyte proliferation.
  • 使用 Everolimus is a semi-synthetic macrocyclic lactone prepared from rapamycin by selective alkylation of the 42-hydroxy group with a silyl-protected hydroxyethyl triflate moiety, followed by addition of an ethylhydroxy moiety to provide greater stability and bioavailability. Like all tacrolimus analogues, everolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. Everolimus is extensively cited in the literature with over 2,000 citations.
  • 定義 ChEBI: A macrocyclic lactone that is rapamycin in which the hydroxy group attached to the cyclohexyl moiety has been converted to the corresponding 2-hydroxyethyl ether. It is an immunosuppressant and antineoplastic agent.
  • brand name Certican
  • Chemical Synthesis Everolimus (IX) was discovered by Sandoz (Novartis) scientists by modifying rapamycin drug in the 40-hydroxyl position. Thus, treatment of rapamycin (84) with t-butyldimethylsilyloxy ethyl triflate in the presence of 2,6-lutidine at 60°C for 3.5 hrs gave ether 85. Deprotection of the silyl group was done by treating silyloxy ether 85 in methanol with 2N HCl to give the product IX (everolimus), which was purified by chromatography. No yields were given for the reactions.

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
Global(380)Suppliers
  • 名前:Wuhan Dujiang Industrial Co., Ltd.
  • 電話番号:+8618120567669 +86-027-87110040
  • ファックス番号:WhatsApp:+86 18120567669
  • 電子メール:wei@dujiangsy.com
  • 国籍:CHINA
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  • 電子メール:sales@tianpharm.com
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  • 国籍:China
  • 製品カタログ:20012
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  • 名前:Beijing Cooperate Pharmaceutical Co.,Ltd
  • 電話番号:010-60279497
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  • 電話番号:008615858145714
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  • 電子メール:fandachem@gmail.com
  • 国籍:CHINA
  • 製品カタログ:8909
  • 優位度:55
159351-69-6, エベロリムス キーワード:
  • 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 fandachem
  • Everolimus USP/EP/BP
  • Everolimus AFINITOR
  • 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)