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Merck
CN
所有图片(1)

主要文件

513036

Sigma-Aldrich

PD 158780

InSolution, ≥95%, EGFR tyrosine kinase activity inhibitor

别名:

InSolution PD 158780

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About This Item

经验公式(希尔记法):
C14H12BrN5
CAS Number:
分子量:
330.18
MDL编号:
UNSPSC代码:
12352200

质量水平

方案

≥95% (HPLC)

表单

liquid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

运输

wet ice

储存温度

−20°C

InChI

1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20)

InChI key

KFHMLBXBRCITHF-UHFFFAOYSA-N

一般描述

A potent inhibitor of the EGFR tyrosine kinase activity (8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC50 =49 nM) and MDA-MB-453 (IC50 = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells.

生化/生理作用

Cell permeable: yes
Primary Target
EGFR
Product competes with ATP.
Reversible: yes
Target IC50: 8 pM against EGFR tyrosine kinase activity; 49 nM, 52 nM, against heregulin-stimulated autophosphorylation in SK-BR-3 and MDA-MB-453 breast carcinomas, respectively

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外形

A 10 mM (500 µg/151 µl) solution of PD 158780 (Cat. No. 513035) in DMSO.

重悬

Following initial thaw, aliquot and freeze (-20°C).

其他说明

Cunnick, J.M., et al. 1998. J. Biol. Chem. 273, 14468.
Rewcastle, G.W., et al. 1998. J. Med. Chem.41, 742.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

10 - Combustible liquids

WGK

WGK 2

闪点(°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

闪点(°C)

87 °C - closed cup - (Dimethylsulfoxide)


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