Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD153035 hydrochloride (ZM 252868) 是有效地EGFR 抑制剂,Ki 和IC50值分别为6和25 pM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 185 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 549 | 现货 | ||
25 mg | ¥ 1,090 | 现货 | ||
50 mg | ¥ 1,920 | 现货 | ||
100 mg | ¥ 3,490 | 现货 | ||
500 mg | ¥ 7,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | PD153035 hydrochloride (ZM 252868) 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. |
靶点活性 | EGFR:5.2 pM(Ki) |
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) |
别名 | ZM 252868 HCl, AG 1517, Tyrphostin AG 1517, SU 5271, PD153035 HCl, ZM 252868 |
分子量 | 396.67 |
分子式 | C16H15BrClN3O2 |
CAS No. | 183322-45-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4 mg/mL (10 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.521 mL | 12.6049 mL | 25.2099 mL | 63.0247 mL |
5 mM | 0.5042 mL | 2.521 mL | 5.042 mL | 12.6049 mL | |
10 mM | 0.2521 mL | 1.2605 mL | 2.521 mL | 6.3025 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PD153035 hydrochloride 183322-45-4 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Inhibitor SU-5271 HER1 ZM 252868 HCl AG 1517 PD-153035 ErbB-1 ZM-252868 Tyrphostin AG 1517 PD153035 Hydrochloride PD-153035 Hydrochloride SU 5271 Epidermal growth factor receptor PD153035 PD153035 HCl SU5271 PD 153035 Tyrphostin AG-1517 ZM252868 inhibit PD 153035 Hydrochloride AG1517 PD-153035 hydrochloride AG-1517 ZM 252868 Tyrphostin AG1517 inhibitor