CCB02

Research use only, not for human use.

CCB02 (CCB 02) is a specific small molecule inhibitor of CPAP-tubulin interaction with IC50 of 0.689 uM in AlphaScreen assay.

CCB02 (CCB 02) is a specific small molecule inhibitor of CPAP-tubulin interaction with IC50 of 0.689 uM in AlphaScreen assay, selectively binds at the CPAP binding site of tubulin; does not inhibits a panel of cell cycle- and centrosome-related kinases; impairs proliferation of cells with centrosome amplification, activates extra centrosomes to nucleate enhanced numbers of microtubules prior to mitosis, causes cells to undergo centrosome de-clustering, prolonged multipolar mitosis, and cell death; demonstrates broad anti-invasive activity in various cancer models, including tyrosine kinase inhibitor (TKI)-resistant EGFR-mutant NSCLC.

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.Cell Viability Assay Cell Line:BT549, MDA-MB-231, Pop10, SCC13, SW1271p53/pRb/CDKN2Adel, KYSE30p53/MYC/CyclinD1, A549G12S, PC-9EGFR-Exon19del, HCC827-GR, HCC1833-GR, H1975T790M cells Concentration:0.1-15 μM Incubation Time:72 hours Result:Exhibited IC50s of 0.86 μM (Pop10), 1.2 μM (HCC827-GR), 1.5 μM (H1975T790Mp53/MYC/CyclinD1), 1.15 μM (HCC1833-GR), 1.61 μM (SW1271p53/pRb/CDKN2Adel), 2.41 μM (SCC13), and 2.94 μM (PC-9EGFR-Exon19del).

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.

CCB 02

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Microtubule/Tubulin

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2100864-57-9

235.246

C14H9N3O

>98% (HPLC)

DMSO : 25 mg/mL 106.27 mM

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

3-methoxybenzo[b][1,6]naphthyridine-4-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years