现货,Saracatinib (AZD0530) ,CAS:379231-04-6,美国进口,受体酪氨酸激酶(RTK),SRC ,SRC 抑制剂和化合物,S1006,selleck

信号转导通路: 受体酪氨酸激酶(RTK) >> SRC >> SRC 抑制剂和化合物 >> Saracatinib (AZD0530)http://selleck.cn/saracatinib-azd0530-S1006.html

技术数据:

分子量(MW): 542.03

化学式:

C27H32ClN5O5

 

溶解度: DMSO ≥108mg/mL Water <1mg/mL Ethanol ≥108mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 379231-04-6

生物活性

 

 

Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively. Saracatinib (AZD0530) a novel anilino quinazoline. AZD0530(Saracatinib) is highly selective for Src and Abl kinases against a large range of tyrosine and serine- threonine kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 µM). Saracatinib (AZD0530) exerts its activity through ATP competitive and reversible inhibition of the target enzyme. Saracatinib (AZD0530) potently inhibited the in vitro proliferation of Src3T3 mouse fibroblasts and demonstrated variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with saracatinib (AZD0530) was observed with IC50 values of 0.2~0.7 µM. In 3-day MTS cell proliferation assays, Saracatinib (AZD0530) inhibited in vitro proliferation of the Bcr–Abl-driven human leukemia cell line K562 with an IC50 of 0.22 µM. In a head-to-head assay measuring EGFR phosphorylation in KB cells, Saracatinib (AZD0530) exhibited an IC50 of 1.25 mM compared with 11 nM for gefitinib. [1][2]

 

 

 

参考文献

Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530 Tim P. Green,Mike Fennell,et al. MOLECULAR ONCOLOGY 2009;3:248–261

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