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CCB02
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CCB02图片
规格:98%
分子量:235.24
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
CCB02是一种选择性的CPAP-tubulin相互作用抑制剂,能够与tubulin结合,竞争β-tubulin的CPAP结合位点,IC50值为689nM,具有高效抗肿瘤活性。CCB02对其他的蛋白没有抑制作用,包括与细胞周期、中心体相关蛋白,同时对AuroraA,Plk1,Plk2,CDK2和CHK1的磷酸化状态无作用。
货号:ajcx12976
CAS:2100864-57-9
分子式:C14H9N3O
分子量:235.24
溶解度:DMSO : 25 mg/mL (106.27 mM)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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[1].

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. CCB02 perturbs CPAP PN2-3-tubulin interaction with an IC50 of 0.441 μM in a PN2-3 CPAP-GST pull-down assay[1].CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1[1].CCB02 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[1].

CCB02 (30 mg/kg, p.o. daily) 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[1].

[1]. Mariappan A, et al. Inhibition of CPAP-tubulin interaction prevents proliferation of centrosome-amplified cancer cells. EMBO J. 2019 Jan 15;38(2). pii: e99876.