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Merck
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安全信息

PZ0020

Sigma-Aldrich

Temsirolimus

≥98% (HPLC)

别名:

42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]-rapamycin, CCI-779

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About This Item

经验公式（希尔记法）:
C56H87NO16
CAS号:
162635-04-3
分子量:
1030.29
MDL编号:
MFCD00934421
UNSPSC代码:
12352200
PubChem化学物质编号:
329823687
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to off-white

溶解性

DMSO: ≥20 mg/mL

储存温度

room temp

SMILES字符串

CO[C@@H]1CC(CC[C@H]1OC(=O)C(C)(CO)CO)C[C@@H](C)[C@@H]2CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](CC3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N4CCCCC4C(=O)O2)OC

InChI

1S/C56H87NO16/c1-33-17-13-12-14-18-34(2)45(68-9)29-41-22-20-39(7)56(67,73-41)51(63)52(64)57-24-16-15-19-42(57)53(65)71-46(30-43(60)35(3)26-38(6)49(62)50(70-11)48(61)37(5)25-33)36(4)27-40-21-23-44(47(28-40)69-10)72-54(66)55(8,31-58)32-59/h12-14,17-18,26,33,35-37,39-42,44-47,49-50,58-59,62,67H,15-16,19-25,27-32H2,1-11H3/b14-12+,17-13+,34-18+,38-26+/t33-,35-,36-,37-,39-,40+,41+,42+,44-,45+,46+,47-,49-,50+,56-/m1/s1

InChI key

CBPNZQVSJQDFBE-FUXHJELOSA-N

基因信息

human ... FKBP1A(2280)

一般描述

Temsirolimus is an esterified rapamycin compound, soluble in water.

应用

Temsirolimus has been used:
  • in combination with radiation to study its effect on von Hippel Lindau (VHL) tumour suppressor gene-deficient renal carcinoma cell lines
  • to induce autophagy
  • as a mammalian target of rapamycin complex 1 (mTORC1) inhibitor to study the effect of cellular Akt-kinase on human papillomaviruses 16 (HPV16) late gene expression

生化/生理作用

Temsirolimus is a specific inhibitor of mammalian target of rapamycin (mTOR) mTOR Complex 1 (mTORC1). Temsirolimus is an antiproliferative and antiangiogenic, the first-in-class mTOR inhibitor approved for the treatment of patients with advanced poor prognosis renal cell carcinoma.
Temsirolimus is an antiproliferative and antiangiogenic mTORC1 inhibitor.
The inhibitory action of temsirolimus is mediated by FKBP-12 (FK506-binding protein 12), a major intracellular protein. It is useful in treating renal-cell carcinoma.

特点和优势

This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

监管及禁止进口产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000357802
0000357802
0000295421
0000295421
0000189194

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C Le Tourneau et al.
British journal of cancer, 99(8), 1197-1203 (2008-09-18)
The proof of principle that a drug targeting mTOR can improve survival has been obtained recently from a large randomised trial using temsirolimus as a first-line therapy in patients with advanced poor prognostic renal cell carcinoma. Consistent data have recently
Viktor Grünwald et al.
European urology, 70(6), 1006-1015 (2016-05-31)
The predictive role of objective remission remains undefined for targeted agents in metastatic renal cell carcinoma (mRCC); however, early tumour shrinkage (eTS) was shown to be predictive and/or prognostic for overall survival (OS) and progression-free survival (PFS) in mRCC in
Temsirolimus
Ma WW and Jimeno A
Drugs Today (Barc), 43(10), 659-669 (2007)
Cynthia Guilbert et al.
PloS one, 8(12), e85995-e85995 (2014-01-07)
Inhibitors of the mammalian target of rapamycin (mTORi) have clinical activity; however, the benefits of mTOR inhibition by rapamycin and rapamycin-derivatives (rapalogs) may be limited by a feedback mechanism that results in AKT activation. Increased AKT activity resulting from mTOR
Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma
Hudes G, et al.
The New England Journal of Medicine, 356(22), 2271-2281 (2007)
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