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替西罗莫司，Temsirolimus；≥98% (HPLC)

别名：雷帕霉素；42-3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate-rapamycin；CCI-779

Empirical Formula (Hill Notation): C56H87NO16 CAS号: 162635-04-3 分子量: 1030.29 MDL编号: MFCD00934421 PubChem化学物质编号: 329823687 NACRES: NA.77

制造商品牌: 西格玛 Sigma-Aldrich

货号（SKU）: PZ0020

CAS号: 162635-04-3

MDL号: MFCD00934421

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目录价.SKU-Variant

5mg
25mg [+$646.55]
100mg [+$1,673.65]

$212.84

数量:

说明

一般描述

Temsirolimus is an esterified rapamycin compound, soluble in water.

是 mTOR 抑制剂，IC50 值为 1.76 μM。Temsirolimus 能激活自噬 (autophagy),在动物模型中防止心脏功能恶化。

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

包装

5, 25 mg in glass bottle

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.

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.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC^®¹²⁸⁰), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC^®^Pfizer), a collection of 90 Pfizer-developed drugs and research tools. Click here to learn more.

其他说明

This compound was developed by Pfizer for Kinase Phosphatase Biology research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

法律信息

Sold for research purposes under agreement from Pfizer Inc.

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Pfizer is a registered trademark of Pfizer, Inc.

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

mfr. no.

Pfizer^®

颜色

white to off-white

溶解性

DMSO: ≥20 mg/mL

创始人

Pfizer

储存温度

room temp

SMILES string

COC@@H1CC(CCC@H1OC(=O)C(C)(CO)CO)CC@@H(C)C@@H2CC(=O)C@H(C)\C=C(C)\C@@H(O)C@@H(OC)C(=O)C@H(C)CC@H(C)\C=C\C=C\C=C(C)\C@H(CC3CCC@@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

Gene Information

human ... FKBP1A(2280)

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格

属性名称	属性值
储存温度 Storage temp.	常温阴凉避光
全球实时库存 Availability √	美国St. Louis ≥ 33 \| 欧洲Eur. ≥ 27 \| 東京Tokyo ≥ 9 \| 香港与北京 ≥ 16

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