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BD5002841

Temsirolimus , 99% , 162635-04-3

Synonym(s):
42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]-rapamycin;CCI-779

CAS NO.:162635-04-3

Empirical Formula: C56H87NO16

Molecular Weight: 1030.29

MDL number: MFCD00934421

EINECS: 686-177-0

Pack Size Price Stock Quantity
100mg RMB2268.80 In Stock
250mg RMB3579.20 In Stock
1g RMB8656.00 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 99-101°C
Boiling point: 1048.4±75.0 °C(Predicted)
Density  1.21
Flash point: 587.8℃
storage temp.  room temp
solubility  Soluble in chloroform, methanol.
pka 10.40±0.70(Predicted)
form  powder
color  white to off-white
Merck  14,9142
InChIKey CBPNZQVSJQDFBE-FUXHJELOSA-N

Description and Uses

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.

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.

Safety

Symbol(GHS) 
GHS08
Signal word  Danger
Hazard statements  H360-H413
Precautionary statements  P501-P273-P202-P201-P280-P308+P313-P405
Safety Statements  24/25
WGK Germany  3
RTECS  VE6257000
HS Code  29349990
Hazardous Substances Data 162635-04-3(Hazardous Substances Data)

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