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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;Certican;Afinitor;Zortress;Everolimus;CERTICAN(R);EveroliMus API;Everolimus powder
CBNumber:
CB9502411
化学式:
C53H83NO14
分子量:
958.232
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
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  T,Xn,F
Rフレーズ  48/25-36-20/21/22-11
Sフレーズ  45-36/37-26-16
RIDADR  UN 1648 3 / PGII
WGK Germany  2
10
HSコード  29349990
絵表示(GHS)
注意喚起語 Danger
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H225 引火性の高い液体および蒸気 引火性液体 2 危険 P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 P264, P280, P305+P351+P338,P337+P313P
H372 長期にわたる、または反復暴露により臓器の障 害 特定標的臓器有害性、単回暴露 1 危険 P260, P264, P270, P314, P501
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(7)

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 エベロリムス
Everolimus
159351-69-6 10mg ¥17500 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01TOC6188
Everolimus
159351-69-6 10mg ¥47000 2018-12-26 購入
Sigma-Aldrich Japan E-068 エベロリムス 溶液 1.0?mg/mL in acetonitrile, ampule of 1?mL, certified reference material
Everolimus solution 1.0?mg/mL in acetonitrile, ampule of 1?mL, certified reference material
159351-69-6 1ml ¥60300 2018-12-25 購入
富士フイルム和光純薬株式会社(wako) W01W0105-0914 エベロリムス(異性体混合物) 97.0+%(HPLC)(異性体混合)
Everolimus (mixture of isomers) 97.0+%(HPLC)(異性体混合)
159351-69-6 25mg ¥48000 2018-12-26 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 50mg ¥42500 2018-12-26 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

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。

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。

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

Macrolide immunosuppressant; derivative of Rapamycin. Inhibits cytokine-mediated lymphocyte proliferation

使用

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM

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

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( 279)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24686 60
Casorganics US Corp
+17326109938
sales@casorganics.com CHINA 175 58
Capot Chemical Co.,Ltd.
+86-571-85586718
+86-571-85864795 sales@capotchem.com China 19921 60
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22631 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 569 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30052 58
Zhejiang ZETian Fine Chemicals Co. LTD
+86-18957127338
sales@zetchem.com CHINA 2886 58

159351-69-6(エベロリムス)キーワード:


  • 159351-69-6
  • Everolimus powder
  • 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine, rapamycin deriv
  • Everolimus solution
  • Everolimus, >=98%
  • 42-O-(2-Hydroxyethyl)-rapamycin
  • Certica
  • Everolimus(mixture of isomers)
  • Rapamycin, 42-O-(2-hydroxyethyl)-
  • Everolimus
  • Certican
  • CERTICAN(R)
  • EveroliMus(RAD-001)
  • RAD-001
  • SDZRAD
  • (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 ada@tuskwei.com whatsapp
  • Everolimus 159351-69-6
  • 40-O-(2-Hydroxyethyl) Rapamycin
  • 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)
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