CCB02

CCB02

C655540-1ml

1ml

10mM in DMSO

充氩,-80℃储存

超低温冰袋运输

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 CHK1 In Vitro CCB02 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 Vivo CCB02 (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)

CCB02是一种选择性CPAP-微管蛋白相互作用抑制剂，能与微管蛋白结合并竞争β-微管蛋白的CPAP结合位点，IC50为689 nM，具有很强的抗肿瘤活性。CCB02对细胞周期和中心体还原没有抑制作用。

2100864-57-9(DMSO)

C14H9N3O

235.24 g/mol

COC1=C(C2=NC3=CC=CC=C3C=C2C=N1)C#N