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Submit ReviewPD 158780
说明： Potent ErbB receptor family inhibitor
化学名： N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
纯度： ≥99% (HPLC)
生物活性 for PD 158780
PD 158780 is a potent inhibitor of ErbB receptor family tyrosine kinases (IC50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells.
化合物库 for PD 158780
PD 158780 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for PD 158780
| 分子量 | 330.18 |
| 公式 | C14H12BrN5 |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 171179-06-9 |
| PubChem ID | 4707 |
| InChI Key | KFHMLBXBRCITHF-UHFFFAOYSA-N |
| Smiles | CNC1=NC=C2N=CN=C(NC3=CC=CC(Br)=C3)C2=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PD 158780
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 33.01 | 100 | |
| ethanol | 8.25 | 25 |
制备储备液 for PD 158780
以下数据基于产品分子量 330.18。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.03 mL | 15.14 mL | 30.29 mL |
| 5 mM | 0.61 mL | 3.03 mL | 6.06 mL |
| 10 mM | 0.3 mL | 1.51 mL | 3.03 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
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产品说明书 for PD 158780
参考文献 for PD 158780
参考文献是支持产品生物活性的出版物。
Fry et al (1997) Biochemical and antiproliferative properties of 4-[ar(alk)ylmino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. Biochem.Pharmacol. 54 877 PMID: 9354588
Sun et al (1999) Growth inhibition of nasopharyngeal carcinoma cells by EGF receptor tyrosine kinase inhibitors. Anticancer Res. 19 919 PMID: 10368634
Gonzales et al (2005) G1 cell cycle arrest due to inhibition of erbB family receptor tyrosine kinases does not require the retinoblastoma protein. Exp.Cell Res. 303 56 PMID: 15572027
If you know of a relevant reference for PD 158780, please let us know.
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关键词: PD 158780, PD 158780 supplier, Potent, ErbB, receptor, family, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, Her, EGFR, Receptor, Tyrosine, Kinases, RTKs, PD158780, 2615, Tocris Bioscience
2 篇 PD 158780 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PD 158780 的部分引用包括：
Ledonne et al (2015) Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons. Mol Psychiatry 20 959 PMID: 25266126
Matsuoka et al (2016) Radial glia regulate vascular patterning around the developing spinal cord. Elife 5 PMID: 27852438
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