CCB02

• CAT Number: I019601
• CAS Number: 2100864-57-9
• Molecular Formula: C14H9N3O
• Molecular Weight: 235.24
• Purity: ≥95%
• Synonyms: 3-methoxybenzo[b][1,6]naphthyridine-4-carbonitrile
• InChI: InChI=1S/C14H9N3O/c1-18-14-11(7-15)13-10(8-16-14)6-9-4-2-3-5-12(9)17-13/h2-6,8H,1H3
• InChIKey: QNJYUHRGCPRPQS-UHFFFAOYSA-N
• SMILES: COC1=C(C2=NC3=CC=CC=C3C=C2C=N1)C#N

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 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 (0.1-15 μM, 72 hours) inhibits the proliferation of cancer cells with extra centrosomes, IC50s are 0.86-2.9 μM[1].
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 for 24 days) shows potent anti-tumor effect in nude mice bearing subcutaneous human lung (H1975T790M cells) tumor xenografts[1].
CCB02 also suppresses MDA-MB-231 cell migration and cuases multipolar mitosis in mouse xenografts[1].

Reference

[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.
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