Home Products Saracatinib (AZD0530)
Saracatinib (AZD0530)
Synonyms: Saracatinib (AZD0530)
CAS NO: 379231-04-6
Molecular Formula: C27H32ClN5O5
Molecular Weight: 542.03
Purity: 98% min
Solubility: In DMSO
Storage: -20°C
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Remarks: 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 exerts its activity through ATP competitive and reversible inhibition of the target enzyme. [1]Saracatinib 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(tumor types: colon, prostate, lung, and leukemia) was observed with IC50 values of 0.2C0.7 µM. In 3-day MTS cell proliferation assays, AZD0530 inhibited in vitro proliferation of the BcrCAbl-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 exhibited an IC50 of 1.25 mM compared with 11 nM for gefitinib.

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