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Home - Products - Cell Cycle/DNA Damage - Aurora Kinase - CCT129202

CCT129202

CAS No. 942947-93-5

CCT129202( CCT-129202 | CCT 129202 )

Catalog No. M16750 CAS No. 942947-93-5

CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CCT129202
  • Note
    Research use only, not for human use.
  • Brief Description
    CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively.
  • Description
    CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively; displays high selectivity for the Aurora kinases over a broad range of 13 other kinases; inhibits proliferation in multiple cultured human tumor cell lines (GI50=0.08-1.7 uM), induces aberrant mitosis that leads to apoptosis; reduces phosphorylation of histone H3, stabilizes p53, and inhibits growth of HCT116 human colon cancer xenografts in athymic mice.
  • In Vitro
    CCT129202 causes the accumulation of human tumor cells with z4N DNA content, leading to apoptosis. CCT129202 is found to induce apoptosis with GI50 values that ranges between 0.08 and 1.7 μM. CCT120202-treated human tumor cells shows a delay in mitosis, abrogation of nocodazole-induced mitotic arrest, and spindle defects. CCT129202 Causes p21Up-regulation, Rb Hypophosphorylation, and H2F-Dependent TK1 Down-regulation.
  • In Vivo
    Growth of HCT116 xenografts in nude mice is inhibited after i.p. administration of CCT129202. p21, the cyclin-dependent kinase inhibitor, is induced by CCT129202. Up-regulation of p21 by CCT129202 in HCT116 cells led to Rb hypophosphorylation and E2F inhibition, contributing to a decrease in thymidine kinase 1 transcription.
  • Synonyms
    CCT-129202 | CCT 129202
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Aurora Kinase
  • Recptor
    Aurora A , Aurora B , Aurora C
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    942947-93-5
  • Formula Weight
    497.0156
  • Molecular Formula
    C23H25ClN8OS
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(NC1=NC=CS1)CN2CCN(C3=C4C(NC(C5=CC=C(N(C)C)C=C5)=N4)=NC=C3Cl)CC2
  • Chemical Name
    1-Piperazineacetamide, 4-[6-chloro-2-[4-(dimethylamino)phenyl]-3H-imidazo[4,5-b]pyridin-7-yl]-N-2-thiazolyl-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Chan F, et al. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57. 2. Cheng C, et al. Mol Pharm. 2012 Jul 2;9(7):1971-82. 3. Tobío A, et al. Antiinflamm Antiallergy Agents Med Chem.
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