2014年8月5日星期二

CYC116|cas 693228-63-6| DC Chem|Supplier|Price|Buy 

CYC116|cas 693228-63-6| DC Chem|Supplier|Price|Buy
DC Chemicals Supply: CYC116|cas 693228-63-6,Purity: >98% ,Cat No. DC7325, In stock.

Contact: website: www.dcchemicals.com,
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CYC116|cas 693228-63-6 ,Synonym: CYC 116; CYC116  ,Chemical name: 4-(2-amino-4-methylthiazol-5-yl)-N-(4-morpholinophenyl)pyrimidin-2-amine ,Molecular Formula: C18H20N6OS ,MW:368.46

CYC116, cas 693228-63-6,Purity: >98%, Best Price and quality from DC Chemicals. CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM.

The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. [1] CYC116 is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that CYC116 has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. [1] In addition, anti-proliferative activity of CYC116 is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis. [1] Mice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. [1]

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