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PD173955
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD173955图片
CAS NO:260415-63-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
PD 173955
PD-173955
产品介绍
PD173955是一种Src激酶家族选择性抑制剂,对Src、Yes和Abl激酶IC50值约为22nM, 对 FGFRα 的效力较低,对InsR和PKC无活性。

产品描述

PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.

体内活性

PD173955作为Src抑制剂,在各类型细胞早期有丝分裂期间有效抑制有丝分裂进程,并诱导不同程度的细胞凋亡。PD173955有效抑制Bcr-Abl依赖性细胞生长,在Bcr-Abl阳性细胞系中IC50为2-35 nM,比Bcr-Abl阴性细胞系灵敏度高约100到200倍。通过抑制试剂盒配体依赖性c-kit自身磷酸化,PD173955也会抑制M07e细胞的试剂盒配体依赖性增殖,IC50为40 nM。

激酶实验

In Vitro Bcr-Abl Kinase Assays: Bcr-Abl complexed to SHIP2 is immunoprecipitated from cell lysates of K562 cells maintained in log-phase culture conditions. Complexes are collected on protein A-Sepharose, and complexes are washed three times in lysis buffer and then washed twice in abl kinase buffer [50 mM Tris (pH 8.0), 10 mM MgCl2, 1 mM DTT, 2 mM p-nitrophenylphosphate, and 2 μM ATP; New England Biolabs Buffer and protocol]. Kinase assays are performed with 10 μM [γ-32P]ATP/sample for 15–60 min at 30°C in the presence or absence of the indicated concentrations of drug. The reaction is stopped by the addition of SDS-PAGE sample buffer and heated at 100°C for 10 min. Proteins are separated on 7.5% SDS-polyacrylamide gels, gels are dried under vacuum, and phosphorylation is visualized by autoradiography on X-ray film.

细胞实验

Cell growth is determined by two methods. For the [3H]thymidine assay, cells (104 cells/well) are cultured in 96-well, round-bottomed plates with diluted DMSO (control) or with varying concentrations of a specific compound that is resuspended in DMSO for 48 h at 37°C. [3H]Thymidine is added at a concentration of 1 μCi/well, and cells are incubated for an additional 18 h. Cells were harvested with the Unifilter system, scintillation fluid (25 μl/well) is added to each well, and [3H]thymidine incorporation is determined on a Packard Scintillation Counter. Data points for all assays are obtained in triplicate, and background incorporation from cell-free wells is determined and subtracted from all data points. For cell viability, control and drug-treated harvested cells are counted on a hemocytometer using the trypan blue dye exclusion method.(Only for Reference)

Cas No.

260415-63-2

分子式

C21H16Cl2N4OS

分子量

443.35

别名

PD 173955;PD-173955

储存和溶解度

DMSO:12 mg/mL (27.1 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years