Temsirolimus

Temsirolimus Struktur
162635-04-3
CAS-Nr.
162635-04-3
Englisch Name:
Temsirolimus
Synonyma:
40-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]-rapamycin;C15182;CS-442;CCL-779;NSC 683864;TEMSIROLIMUS;Simultaneous;TeMsiroliMus (~90%);Temsirolimus, >=98%;CCI-779; NSC 683864
CBNumber:
CB3506811
Summenformel:
C56H87NO16
Molgewicht:
1030.29
MOL-Datei:
162635-04-3.mol

Temsirolimus Eigenschaften

Schmelzpunkt:
99-101°C
Siedepunkt:
1048.4±75.0 °C(Predicted)
Dichte
1.21
Flammpunkt:
587.8℃
storage temp. 
room temp
Löslichkeit
Soluble in chloroform, methanol.
pka
10.40±0.70(Predicted)
Aggregatzustand
powder
Farbe
white to off-white
Merck 
14,9142
InChIKey
CBPNZQVSJQDFBE-FUXHJELOSA-N
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
S-Sätze: 24/25
WGK Germany  3
RTECS-Nr. VE6257000
HS Code  29349990
Giftige Stoffe Daten 162635-04-3(Hazardous Substances Data)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H360 Kann die Fruchtbarkeit beeinträchtigen oder das Kind im Mutterleib schädigen. Fertility (Fruchtbarkeit) Kategorie 1 Achtung GHS hazard pictogramssrc="/GHS08.jpg" width="20" height="20" />
H413 Kann für Wasserorganismen schädlich sein, mit langfristiger Wirkung. Langfristig (chronisch) gewässergefährdend Kategorie 4
Sicherheit
P201 Vor Gebrauch besondere Anweisungen einholen.
P202 Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.
P273 Freisetzung in die Umwelt vermeiden.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P308+P313 BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.
P405 Unter Verschluss aufbewahren.

Temsirolimus Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Chemische Eigenschaften

White Solid

Verwenden

Temsirolimus, a cell cycle inhibitor developed by Wyeth for the treatment of renal cell carcinoma, was launched in the US in 2007. Temsirolimus works by inhibiting mTOR (mammalian target of rapamycin)-driven cell proliferation. Temsirolimus is also being developed for the treatment of mantle cell lymphoma (PhIII) and also as mono- or combination therapy for the treatment of ovarian and endometrium cancer (PhII). Additionally, temsirolimus is being evaluated for the treatment of several other types of cancer as well as multiple sclerosis and rheumatoid arthritis.

Allgemeine Beschreibung

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.

Temsirolimus Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Temsirolimus Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 266)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hebei Mojin Biotechnology Co., Ltd
+8613288715578
sales@hbmojin.com China 12456 58
Henan Bao Enluo International TradeCo.,LTD
+86-17331933971 +86-17331933971
deasea125996@gmail.com China 2503 58
Ouhuang Engineering Materials (Hubei) Co., Ltd
+8617702722807
admin@hbouhuang.com China 2259 58
Shanghai Daken Advanced Materials Co.,Ltd
+86-371-66670886
info@dakenam.com China 15928 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21691 55
Hangzhou FandaChem Co.,Ltd.
008657128800458; +8615858145714
fandachem@gmail.com China 9348 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 - 03@
sales03@shyrchem.com CHINA 738 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32480 60
career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29914 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 967 58

162635-04-3()Verwandte Suche:


  • 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropa
  • Temsirolimus(CCI-779)
  • TEMSIROLIMUS
  • CCL-779
  • Rapamycin 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate
  • TeMsiroliMus (CCI-779, Torisel)
  • rapaMycin 42-ester with 3-hydroxy-2-(hydroxyMethyl)-2-Methylpropionic acid
  • 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]rapamycin
  • C15182
  • 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
  • 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
  • Temsirolimus (mixture of isomers)
  • Temsirolimus USP/EP/BP
  • TemsirolimusQ: What is Temsirolimus Q: What is the CAS Number of Temsirolimus Q: What is the storage condition of Temsirolimus Q: What are the applications of Temsirolimus
  • 162635-04-3 Temsirolimus
  • temsirolimus 162635-04-3
  • CCI-779; NSC 683864
  • CS-442
  • Simultaneous
  • 40-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]-rapamycin
  • (1R,2R,4R)-4-((R)-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]oxa[4]azacyclohentriacontin-3-yl)propyl)-2-methoxycyclohexyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
  • 162635-04-3
  • 475271-62-2
  • C56H87NO16
  • Antineoplastic protein kinase inhibitors
  • mTOR inhibitor
  • Anti-cancer&immunity
  • PI3K/Akt/mTOR
  • CCI-779, NSC 683864
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
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