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编 号:F269898
分子式:C14H9N3O
分子量:235.24
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1.

体内研究:
CCB02 (30 mg/kg, p.o. daily for 24 days) shows potent anti-tumor effect in nude mice bearing subcutaneous human lung (H1975T790M cells) tumor xenografts.CCB02 also suppresses MDA-MB-231 cell migration and cuases multipolar mitosis in mouse xenografts.Animal Model:Nude mice bearing subcutaneous human lung (H1975T790M) tumor xenografts
Dosage:30 mg/kg
Administration:P.O. daily for 24 days
Result:Significantly decreased the tumor volume on day 24.

体外研究:
CCB02 perturbs CPAP PN2-3-tubulin interaction with an IC50 of 0.441 μM in a PN2-3 CPAP-GST pull-down assay.CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1.CCB02 (0.1-15 μM, 72 hours) inhibits the proliferation of cancer cells with extra centrosomes, IC50s are 0.86-2.9 μM. CCB02 activates spindle assembly checkpoint, induces PCM proteins recruitment to centrosomes, and enhances microtubule nucleation activities of centrosomes.
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