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PD153035 hydrochloride
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。
PD153035 hydrochloride图片
CAS NO:183322-45-4
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Tyrphostin AG 1517
PD153035 HCl
ZM 252868 HCl
AG 1517
SU 5271
ZM 252868
产品介绍
PD153035 Hydrochloride 是有效地EGFR抑制剂,Ki和IC50值分别为6和25 pM。

产品描述

PD153035 hydrochloride (ZM 252868; AG 1517) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src.

体外活性

作用于HFD-fed小鼠时,PD153035促进耐糖量、胰岛素敏感性和信号,并使亚临床炎症降低.作用于携带A431人体表皮样癌细胞移植瘤的免疫缺陷裸鼠,PD153035(80 mg/kg)对EGF受体酪氨酸激酶活性有抑制作用.

体内活性

PD153035剂量依赖性地抑制鼻咽癌细胞系HONE1(IC50:18.6 μM),NPC-TW04(IC50:9.8 μM)和NPC-TW01(IC50:12.9 μM)。PD153035抑制A-431人扁平上皮癌相关的表皮生长因子受体酪氨酸激酶(Ki:5.2 pM,IC50:29 pM)。作用于Caco-2结肠癌细胞时,PD153035可使PAR(2)激活肽2-呋喃甲酰基-LIGRLO-NH(2)(2fLI)诱导的COX-2表达沉默。作用于Swiss 3T3成纤维细胞和A-431人扁平上皮癌细胞时,PD153035可选择性抑制EGF诱导的酪氨酸磷酸化(IC50:15 nM和14 nM)。作用于过量表达EGF受体的人癌细胞系时,PD153035抑制包括A431, DU145, Difi, ME180和MDA-MB-468在内的细胞生长,IC50分别为0.22 μM, 0.4 μM, 0.3 μM, 0.95 μM和0.68 μM。

激酶实验

Inhibition of EGF receptor tyrosine kinase : Enzyme reactions are performed in a total volume of 0.1 mL containing 25 mM Hepes (pH 7.4), 5 mM MgCl2, 2 mM MnCl2, 50 μM sodium vanadate, 0.5 to 1.0 ng of enzyme (which also contains enough EGF to make the final concentrations 2 μg/mL), 10 μM ATP containing 1 μCi of [32P]ATP, varying concentrations of PD153035, and 200 μM of a substrate peptide based on a portion of phospholipase C-γl having the sequence Lys-His-Lys-Lys-Leu-Ala-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. The reaction is initiated by the addition of ATP. After 10 minutes at room temperature, the reaction is terminated by addition of 2 mL of 75 mM phosphoric acid, and the solution is passed through a 2.5-cm phosphocellulose filter disk that binds the peptide. The filter is washed five times with 75 mM phosphoric acid and placed in a vial with 5 mL of scintillation fluid. The uninhibited control activity produces approximately 100,000 cpm.

细胞实验

Cells are seeded in sixwell plates. The next day, cells are changed to medium containing 0.5% FBS for 18 hours, and then PD153035 is added at various concentrations to the cultures. After 72 hours of treatment, cells are washed once with PBS, harvested with 0.1% human trypsin-l mM EDTA in PBS, and counted with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.(Only for Reference)

Cas No.

183322-45-4

分子式

C16H15BrClN3O2

分子量

396.67

别名

Tyrphostin AG 1517;PD153035 HCl;ZM 252868 HCl;AG 1517;SU 5271;ZM 252868

储存和溶解度

DMSO:4 mg/mL (10 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years