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Submit ReviewGW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 values are 0.01 and 0.014 μM respectively). Selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 values are 0.11 μM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μM for inhibition of non-tumor cell line HFF). Inhibits tumor growth in vivo by ~ 80% in a murine xenograft model following oral administration.
Sold for research purposes under agreement from GlaxoSmithKline.
GW 583340 dihydrochloride is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 671.03 |
公式 | C28H25ClFN5O3S2.2HCl |
储存 | Desiccate at +4°C |
纯度 | ≥97% (HPLC) |
CAS Number | 1173023-85-2 |
PubChem ID | 16219404 |
InChI Key | WIMITXDBYLKRKB-UHFFFAOYSA-N |
Smiles | Cl.Cl.CS(=O)(=O)CCNCC1=NC(=CS1)C1=CC=C2N=CN=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 67.1 | 100 温和加热 |
以下数据基于产品分子量 671.03。 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 | 1.49 mL | 7.45 mL | 14.9 mL |
5 mM | 0.3 mL | 1.49 mL | 2.98 mL |
10 mM | 0.15 mL | 0.75 mL | 1.49 mL |
50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
参考文献是支持产品生物活性的出版物。
Gaul et al (2003) Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines. Bioorg.Med.Chem.Lett. 13 637 PMID: 12639547
If you know of a relevant reference for GW 583340 dihydrochloride, please let us know.
关键词: GW 583340 dihydrochloride, GW 583340 dihydrochloride supplier, Potent, dual, EGFR, ErbB2, inhibitors, inhibits, orally, active, Epidermal, Growth, Factors, Receptors, Her, Receptor, Tyrosine, Kinases, RTKs, GW583340, dihydrochloride, GlaxoSmithKline, GSK, 2239, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GW 583340 dihydrochloride 的部分引用包括:
Sodani et al (2012) GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. Biochem Pharmacol 83 1613 PMID: 22414725
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