化合物PD153035 hydrochloride T1761

Product Introduction
Bioactivity


英文名: PD153035 hydrochloride

描述: PD153035 hydrochloride (ZM 252868) 是有效地EGFR 抑制剂，Ki 和IC50值分别为6和25 pM。

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)

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.

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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4 mg/mL (10 mM)


关键字: Inhibitor | SU-5271 | HER1 | PD-153035 | ErbB-1 | PD153035 hydrochloride | ZM-252868 | PD153035 Hydrochloride | PD-153035 Hydrochloride | Epidermal growth factor receptor | PD153035 | SU5271 | PD 153035 | Tyrphostin AG-1517 | ZM252868 | EGFR | inhibit | PD 153035 Hydrochloride | AG1517 | PD-153035 hydrochloride | AG-1517 | Tyrphostin AG1517

相关产品: Methyl 2,5-dihydroxycinnamate | Dacomitinib | EGFR-IN-8 | TAK-285 | O-Desmethyl gefitinib | CGP77675 | Simotinib | MAPK-IN-2 | E-4031 | SKLB 1028

相关库: Anti-Liver Cancer Compound Library | Angiogenesis related Compound Library | Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Reprogramming Compound Library

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