产品
编 号:F746532
分子式:C41H42Cl2N6O4
分子量:753.72
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1mg
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5mg
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10mg
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生物活性:
S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. S65487 hydrochloride is also active on BCL-2 mutations, such as G101V and D103Y. S65487 hydrochloride has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 hydrochloride induces apoptosis and has anticaner activities.

体内研究:
S65487 hydrochloride induces complete regression in BCL-2-dependent RS4;11 tumors in vivo after a single IV (intravenous) administration. Strong and persistent tumor regression in xenograft models of lymphoid malignancies in mouse and rat are observed at well tolerated doses following weekly IV administration of S65487 hydrochloride in combination with the MCL-1-specific inhibitor, S64315/MIK665.

体外研究:
S65487 hydrochloride binds to the BH3 hydrophobic groove of BCL-2. S65487 hydrochloride induces apoptosis in a panel of hematological cancer cell lines and inhibits cell proliferation with IC50s in the low nM range.
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