1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin
  3. CCB02

CCB02 

Cat. No.: HY-114302
Handling Instructions

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.

For research use only. We do not sell to patients.

CCB02 Chemical Structure

CCB02 Chemical Structure

CAS No. : 2100864-57-9

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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].

IC50 & Target

IC50: 689 nM (CPAP-tubulin)[1]

In Vitro

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].

Cell Viability Assay[1]

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).
In Vivo

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].

Animal Model: Nude mice bearing subcutaneous human lung (H1975T790M) tumor xenografts[1]
Dosage: 30 mg/kg
Administration: P.O. daily for 24 days
Result: Significantly decreased the tumor volume on day 24.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (106.27 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2510 mL 21.2549 mL 42.5098 mL
5 mM 0.8502 mL 4.2510 mL 8.5020 mL
10 mM 0.4251 mL 2.1255 mL 4.2510 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

235.24

Formula

C₁₄H₉N₃O

CAS No.

2100864-57-9

SMILES

N#CC1=C(OC)N=CC2=CC3=CC=CC=C3N=C12

Shipping

Room temperature in continental US; may vary elsewhere

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CCB02
Cat. No.:
HY-114302
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CCB02

Cat. No.: HY-114302