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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Cell Cycle>Aurora Kinase Inhibitors>CCT129202
CCT129202
  • CCT129202

CCT129202 NEW

Price $39 $54 $81
Package 1mg 2mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-14

Product Details

Product Name: CCT129202 CAS No.: 942947-93-5
Purity: 98.14% Supply Ability: 10g
Release date: 2024/11/14

Product Introduction

Bioactivity

名稱CCT129202
描述CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.
細(xì)胞實(shí)驗(yàn)Cells are treated with a range of 0 to 50 uM of CCT129202 for 72 hours. Cell proliferation is analyzed with the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The absorbance is measured at 570 nm using the Wallac VICTOR2TM 1420 Multilabel Counter.(Only for Reference)
激酶實(shí)驗(yàn)Inhibition of Aurora Kinases: NH2-terminal glutathione S-transferase (GST)-fusion recombinant human Aurora A (aa 118-403), Aurora B (full length), and Aurora C (full length) are expressed in baculovirus, purified, and used in the kinase inhibition assays. The in vitro kinase assays are performed in kinase buffer (50 mM Tris pH 7.5, 10 mM NaCl, 2.5 mM MgCl2 and 1 mM DTT) containing γ-32P-ATP, Aurora kinase and different concentrations of CCT129202. The reactions are incubated for 30 minutes at 30 °C and stopped by adding sample buffer. The reactions are separated on Novex Tris-Glycine gels and dried on a vacuum gel drier at 80 °C for 1 hour before exposure to Kodak-Biomax XR film. The concentration of CCT129202 that inhibits Aurora kinases by 50% is calculated representing IC50 value.
體外活性CCT129202 is an ATP-competitive inhibitor of recombinant Aurora A kinase with a Ki of 49.8 nM. CCT129202 at 1 μM shows high selectivity for Aurora A and Aurora B with 92% and 60% inhibition, respectively. It inhibits FGFR3 slightly by 27%, and is not active against CRAF. CCT129202 inhibits proliferation in multiple cultures of human tumor cell lines with half-maximal growth inhibition (GI50) values ranging from 0.08 μM for MV4-11 to 1.7 μM for MDA-MB-157. The effects are in association with increased expression levels of Aurora A and Aurora B leading to aberrant mitosis. Treatment with CCT129202 (0.7 μM) causes the accumulation of HCT116 cells with ≥4N DNA content, leading to apoptosis in a time dependent manner. Application of CCT129202 in HCT116 cells causes decreased histone H3 phosphorylation and increased p53 protein stabilization, which are consistent with the inhibition of Aurora B and Aurora A, respectively. CCT129202 induces up-regulation of p21 in HCT116, HT29 and Hela cells in a p53 dependent and independent manner, which leads to decreased phosphorylation of the Rb protein and activity of E2F in a concentration-dependent manner. [1]
體內(nèi)活性Administration of CCT129202 at 100 mg/kg in athymic mice bearing s.c. HCT116 colon cancer xenografts causes ~50% reduction of histone H3 phosphorylation after 30 minutes of treatment, and significantly inhibits tumor growth by 57.7% compared to control mice after a period of 9 days of treatment. [1]
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 4.97 mg/mL (10 mM)
關(guān)鍵字inhibit | Inhibitor | Aurora Kinase | CCT129202 | CCT 129202 | CCT-129202
相關(guān)產(chǎn)品Palmatine chloride | MK-8745 | SC-514 | Barasertib-HQPA | MBM-55S | SP600125 | KW-2449 | Palmatine | Alisertib | TAK-901 | Tozasertib | TCS7010
相關(guān)庫經(jīng)典已知活性庫 | 表觀遺傳庫 | 激酶抑制劑庫 | 抑制劑庫 | 已知活性化合物庫 | 臨床前化合物庫 | 抗癌化合物庫 | 抗癌活性化合物庫

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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