ChemicalBook--->CAS DataBase List--->2100864-57-9

2100864-57-9

2100864-57-9 Structure

2100864-57-9 Structure
IdentificationBack Directory
[Name]

CCB02
[CAS]

2100864-57-9
[Synonyms]

CCB02
CCB-02,CCB02
Benzo[b][1,6]naphthyridine-4-carbonitrile, 3-methoxy-
[Molecular Formula]

C14H9N3O
[MOL File]

2100864-57-9.mol
[Molecular Weight]

235.24
Chemical PropertiesBack Directory
[Boiling point ]

467.2±25.0 °C(Predicted)
[density ]

1.33±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 25 mg/mL (106.27 mM)
[form ]

Solid
[pka]

2.53±0.30(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Description]

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].

[References]

[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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