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CAS No.: 171179-06-9

PD 158780 Catalog No. CSN13798

Synonyms: PD158780

PD158780, a pyridopyrimidine derivative, is reversible inhibitor of ErbB receptor family (IC50s for EGFR, ErbB2 and ErbB2/ErbB4 are 0.008 nM, 49 nM and 52 nM respectively).

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:0.08nM
描述Epidermal growth factor (EGF) signaling is well known to involve in tumor survival and overexpression of EGF receptor (EGF-R) attributes to decreased responsiveness to many available therapies in cancer treatment^[3]. PD158780 is a potent EGFR family inhibitor with IC50s of 8 uM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively^[4]. At low concentrations, PD158780 inhibited keratinocyte migration directionality, but not the rate of migration; at higher concentrations, it reduced the migration rate as well^[5]. PD158780 potently inhibited the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGF receptor tyrosine phosphorylation in HeLa cells, while it had no detectable effect on c-Src kinase activity. PD158780 also inhibited LPA-induced MKK1/2 activation and DNA synthesis in NIH 3T3 cells^[6]. PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels^[4].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0286 mL
- 15.1431 mL
- 30.2863 mL
- 5 mM
- 0.6057 mL
- 3.0286 mL
- 6.0573 mL
- 10 mM
- 0.3029 mL
- 1.5143 mL
- 3.0286 mL

技术信息

CAS号

171179-06-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H12BrN5

运输

蓝冰

分子量

330.18

别名

PD158780

溶解度

DMSO	21.0 mg/mL (63.6 mM)

动物实验配方

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