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Merck
CN

PZ0020

Sigma-Aldrich

Temsirolimus

≥98% (HPLC)

别名:

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

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关于此项目

经验公式（希尔记法）:
C56H87NO16
化学文摘社编号:
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

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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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hnRNP L controls HPV16 RNA polyadenylation and splicing in an Akt kinase-dependent manner
Kajitani N, et al.
Nucleic Acids Research, 45(16), 9654-9678 (2017)
Radiosensitization of renal cell carcinoma in vitro through the induction of autophagy
Anbalagan S, et al.
Radiotherapy and Oncology : Journal of the European Society for Therapeutic Radiology and Oncology, 103(3), 388-393 (2012)
Meng Ling Choong et al.
Journal of cellular and molecular medicine, 17(11), 1397-1409 (2013-11-21)
Current JAK2 inhibitors used for myeloproliferative neoplasms (MPN) treatment are not specific enough to selectively suppress aberrant JAK2 signalling and preserve physiological JAK2 signalling. We tested whether combining a JAK2 inhibitor with a series of serine threonine kinase inhibitors, targeting
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)
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实验方案

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