CCB02 (C09-1121-155)

CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC 50 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 CHK1In VitroCCB02 perturbs CPAP PN2-3-tubulin interaction with an IC 50 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, IC 50 s are 0.86-2.9 μM. CCB02 activates spindle assembly checkpoint, induces PCM proteins recruitment to centrosomes, and enhances microtubule nucleation activities of centrosomes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: BT549, MDA-MB-231, Pop10, SCC13, SW1271 p53/pRb/CDKN2Adel , KYSE30 p53/MYC/CyclinD1 , A549 G12S , PC-9 EGFR-Exon19del , HCC827-GR, HCC1833-GR, H1975 T790M cells Concentration: 0.1-15 μM Incubation Time: 72 hours Result: Exhibited IC 50 s of 0.86 μM (Pop10), 1.2 μM (HCC827-GR), 1.5 μM (H1975 T790Mp53/MYC/CyclinD1 ), 1.15 μM (HCC1833-GR), 1.61 μM (SW1271 p53/pRb/CDKN2Adel ), 2.41 μM (SCC13), and 2.94 μM (PC-9 EGFR-Exon19del ).In VivoCCB02 (30 mg/kg, p.o. daily for 24 days) shows potent anti-tumor effect in nude mice bearing subcutaneous human lung (H1975 T790M cells) tumor xenografts . CCB02 also suppresses MDA-MB-231 cell migration and cuases multipolar mitosis in mouse xenografts . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.IC50& Target:IC50: 689 nM (CPAP-tubulin). Specification: 10mM in DMSO Molecular Formula: C14H9N3O Molecular Weight: 235.24