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CCB02

カタログ番号GC33300 Copy One-Click Copy Product Info

CCB02 は選択的 CPAP-チューブリン相互作用阻害剤であり、チューブリンに結合し、β-チューブリンの CPAP 結合部位と競合し、IC50 は 689 nM であり、強力な抗腫瘍活性を示します。 CCB02 は、細胞周期および中心体関連のキナーゼ、または Aurora A、Plk1、Plk2、CDK2、および CHK1 のリン酸化状態を阻害しません。

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CCB02 化学構造

Cas No.: 2100864-57-9

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Sample solution is provided at 25 µL, 10mM.



Description of CCB02

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.

Chemical Properties of CCB02

Cas No. 2100864-57-9 SDF
Canonical SMILES N#CC1=C(OC)N=CC2=CC3=CC=CC=C3N=C12
Formula C14H9N3O M.Wt 235.24
溶解度 DMSO : 25 mg/mL (106.27 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CCB02

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1 mg 5 mg 10 mg
1 mM 4.251 mL 21.2549 mL 42.5098 mL
5 mM 850.2 μL 4.251 mL 8.502 mL
10 mM 425.1 μL 2.1255 mL 4.251 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Average Rating: 5 ★★★★★ (Based on Reviews and 16 reference(s) in Google Scholar.)

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