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テムシロリムス

テムシロリムス 化学構造式
162635-04-3
CAS番号.
162635-04-3
化学名:
テムシロリムス
别名:
テムシロリムス;ラパマイシン42-[3-ヒドロキシ-2-(ヒドロキシメチル)-2-メチルプロパノアート];テムシロリムス (〜90%);テムシロリムス(異性体混合物);テムシロリムス (CCI-779, Torisel);テムシロリムス (JAN)
英語化学名:
Temsirolimus
英語别名:
C15182;CS-442;CCL-779;NSC 683864;TEMSIROLIMUS;Simultaneous;Temsirolimus, >=98%;CCI-779; NSC 683864;TeMsiroliMus (~90%);Temsirolimus(CCI-779)
CBNumber:
CB3506811
化学式:
C56H87NO16
分子量:
1030.29
MOL File:
162635-04-3.mol

テムシロリムス 物理性質

融点 :
99-101°C
沸点 :
1048.4±75.0 °C(Predicted)
比重(密度) :
1.21
闪点 :
587.8℃
貯蔵温度 :
-20°C Freezer
溶解性:
Soluble in chloroform, methanol.
酸解離定数(Pka):
10.40±0.70(Predicted)
外見 :
powder
色:
white to off-white
Merck :
14,9142
InChIKey:
CBPNZQVSJQDFBE-FUXHJELOSA-N

安全性情報

Sフレーズ  24/25
WGK Germany  3
RTECS 番号 VE6257000
HSコード  29349990

テムシロリムス 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) W01TOC5264
Temsirolimus
162635-04-3 10mg ¥44000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01BVI1600-5
Temsirolimus (CCI-779, Torisel)
162635-04-3 5mg ¥72800 2018-12-26 購入
東京化成工業 T3574 テムシロリムス >95.0%(HPLC)
Temsirolimus >95.0%(HPLC)
162635-04-3 50mg ¥39900 2018-12-04 購入
東京化成工業 T3574 テムシロリムス >95.0%(HPLC)
Temsirolimus >95.0%(HPLC)
162635-04-3 10mg ¥11400 2018-12-04 購入
Sigma-Aldrich Japan PZ0020 ≥98% (HPLC)
Temsirolimus ≥98% (HPLC)
162635-04-3 5mg ¥24700 2018-12-25 購入

テムシロリムス 化学特性,用途語,生産方法

外観

白色~わずかにうすい褐色、結晶~粉末

溶解性

エタノール(99.5)に溶けやすく、水にほとんど溶けない。

用途

mTOR 阻害剤で、乳がん細胞株において腫瘍の成長を阻害します(IC50=1.6 nmol/l(SKBr3),4.3 nmol/l(BT474))。

効能

抗悪性腫瘍薬, mTOR阻害薬

商品名

トーリセル (ファイザー)

説明

While renal cell carcinoma (RCC) accounts for only 2 3% of all cancers, the 5-year survival rate for advanced RCC disease is only 5 10%, with approximately 13,000 deaths occurring annually (US statistics only). Immunotherapeutic cytokine options, such as IFN-αand IL-2, have traditionally been frontline treatments, but these agents are not efficacious in all patients and can cause serious side effects. In addition, bevacizumab, a monoclonal antibody against VEGF, has also demonstrated prolongation of PFS. The newest entry for this indication focuses on targets that are downstream from VEGF. Temsirolimus is an inhibitor of the serine/threonine kinase mTOR, which is the mammalian target of rapamycin. mTOR has been implicated in cell replication through control of the cell cycle translation of specific mRNAs. Inhibition of mTOR prevents phosphorylation of the 4E binding protein-1 and the 40S ribosomal protein S6 kinase that are responsible for cell cycle protein translation initiation; cell cycle arrest occurs as the result of termination of cell division from the G1 to the S phase. Disruption of mTOR signaling also has antiangiogenic effects that could be deemed essential in combating RCC, which is driven by unregulated angiogenesis. Temsirolimus is the 2,2-bis(hydroxymethyl)propionate ester of rapamycin (sirolimus), a macrolide fungicide isolated from the bacteria Streptomyces hygroscopicus. Similar to its parent sirolimus, temsirolimus interacts with mTOR through its complex with FK-506 binding protein 12.

化学的特性

White Solid

Originator

Wyeth (US)

使用

Ester analog of Rapamycin

使用

Temsirolimus (CCI-779) is a specific mTOR inhibitor with IC50 of 1.76 μM.

使用

Temsirolimus is a semisynthetic macrocyclic lactone prepared from rapamycin by selective alkylation of the 42-hydroxy group with a protected bis(dihydromethyl)propionic acid, followed by deprotection. Like all tacrolimus analogues, temsirolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. Temsirolimus is extensively cited in the literature with over 700 citations.

使用

Temsirolimus is a semisynthetic macrocyclic lactone prepared from rapamycin by selective acylation of the 42-hydroxy group with a protected bis(dihydromethyl)propionic acid, followed by deprotection. Like all tacrolimus analogues, temsirolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. Temsirolimus is extensively cited in the literature with over 700 citations.

brand name

Torisel

一般的な説明

Temsirolimus is an esterified derivative of rapamycinand in a similar manner binds initially to the proteinFKBP-12(FK506-binding protein).This complexthen acts to inhibit the mammalian target of rapamycin(mTOR), a serine-threonine kinase that plays a crucial rolein cell division. It is somewhat unique in its method of kinaseinhibition, because it actually binds to an allostericmodulator of the kinase rather than just binding to theATP-binding site like most other kinase inhibitors.Temsirolimus is available as a 25-mg/mL injection forIV administration in the treatment of advanced RCC. Theagent is extensively metabolized and undergoes rapid hydrolysisof the ester function to give rapamycin that retainsactivity.Additional metabolism is mediated primarilyby CYP3A4 to give several hydroxylated and demethylatedmetabolites that are inactive. The agent and metabolites areeliminated primarily in the feces with half-lives of 17 and55 hours for temsirolimus and rapamycin, respectively.This agent, like rapamycin, possesses immunosuppressantproperties and there is an increased risk of infection.The most serious side effects are interstitial lung disease,perforation of the bowel, and acute renal failure althoughthese occur only rarely. The most commonly seen side effects are rash, weakness, mucositis, nausea, edema, andanorexia.

Chemical Synthesis

While rufinamide may be prepared by several related routes, the preferred starting material is 2,6-difluorobenzyl azide. Reaction with either 2-propynoic acid or 2-chloroacrylonitrile affords 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid or 1-(2,6-difluorobenzyl)- 1H-1,2,3-triazole-4-carbonitrile, respectively. For the carboxylic acid Shridhar Hegde and Michelle Schmidt intermediate, treatment with thionyl chloride followed by concentrated aqueous ammonium hydroxide or conversion to its methyl ester (methanol/sulfuric acid) with subsequent ammonolyis provides rufinamide.

テムシロリムス 上流と下流の製品情報

原材料

準備製品


テムシロリムス 生産企業

Global( 171)Suppliers
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Henan DaKen Chemical CO.,LTD.
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Henan Tianfu Chemical Co.,Ltd.
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Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
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ATK CHEMICAL COMPANY LIMITED
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162635-04-3(テムシロリムス)キーワード:


  • 162635-04-3
  • CCI-779; NSC 683864
  • Temsirolimus, >=98%
  • NSC 683864
  • (1R,2R,4S)-4-{(2R)-2-[(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontin-3-yl]propyl}-2-methoxycyclohexyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
  • 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropa
  • 40-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]-rapamycin
  • Temsirolimus(CCI-779)
  • TEMSIROLIMUS
  • CCL-779
  • Rapamycin 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate
  • 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]rapamycin
  • C15182
  • TeMsiroliMus (CCI-779, Torisel)
  • rapaMycin 42-ester with 3-hydroxy-2-(hydroxyMethyl)-2-Methylpropionic acid
  • TeMsiroliMus (Torisel)
  • TeMsiroliMus (~90%)
  • TeMsiroliMus (Torisel,CCI-779,NSC-683864)
  • TeMsiroliMus (CCI-779, NSC 683864)
  • Rapamycin 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate Temsirolimus
  • Temsirolimus Rapamycin 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
  • 42-[3-Hydroxy-2-methylpropanoate
  • Simultaneous
  • temsirolimus 162635-04-3
  • CS-442
  • テムシロリムス
  • ラパマイシン42-[3-ヒドロキシ-2-(ヒドロキシメチル)-2-メチルプロパノアート]
  • テムシロリムス (〜90%)
  • テムシロリムス(異性体混合物)
  • テムシロリムス (CCI-779, Torisel)
  • テムシロリムス (JAN)
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