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ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  DNA damage >  ATM / ATR inhibitor >  2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE

2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE

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2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE Basic information

Product Name:
2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE
Synonyms:
  • CS-713
  • CGK-733; CGK 733
  • ATM/ATR Kinase Inhibitor - CAS 905973-89-9 - Calbiochem
  • 2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE
  • CGK733
  • A-PHENYL-N-[2,2,2-TRICHLORO-1-[[[(4-FLUORO-3-NITROPHENYL)AMINO]THIOXOMETHYL]AMINO]ETHYL]BENZENEACETAMIDE
  • α-Phenyl-N-[2,2,2-trichloro-1-[[[(4-fluoro-3-nitrophenyl)amino]thioxomethyl]amino]ethyl]benzeneacetamide
  • alpha-Phenyl-N-[2,2,2-trichloro-1-[[[(4-fluoro-3-nitrophenyl)amino]thioxomethyl]amino]ethyl]-benzeneacetamide
CAS:
905973-89-9
MF:
C23H18Cl3FN4O3S
MW:
555.84
Product Categories:
  • Inhibitors
Mol File:
905973-89-9.mol
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2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE Chemical Properties

storage temp. 
Sealed in dry,2-8°C
form 
Pale yellow solid
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2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE Usage And Synthesis

Uses

CGK733 is a noted ataxia telangiectasia-mutated (ATM) protein/kinase inhibitor. Cell proliferation inhibitor and anticancer agent.

Uses

Ataxia-telangiectasia mutated (ATM) and ATM- and Rad3-related (ATR) kinases mediate the DNA damage response pathway in cells upon encounter with genotoxic agents. Their signaling can activate cell cycle arrest, DNA repair, induction of premature senescence, and cell death. Inhibiting this pathway is one strategy implemented to increase the therapeutic capacity of certain genotoxic anti-cancer regimens by sensitizing cancer cells to these agents. CGK733, a thiourea-containing compound, was originally identified as a specific inhibitor of ATR and ATM kinases (IC50 = ~ 200 nM). In prematurely senescent breast, lung, and colon cancer cells CGK733 reportedly suppresses ATM-mediated p21 expression required for survival, resulting in cell death. Human cancer cell lines exposed to both caffeine and CGK733 demonstrate a rapid decline in cyclin D1 protein levels and a reduction in retinoblastoma protein levels, which leads to the inhibition of their proliferation.

Biological Activity

Originally defined as a selective inhibitor of ATR and ATM kinases that reverses senescence in human BJ and HMEC cells. Decreases p21 CIP1 levels in senescent with no effect on p53 and Bcl-2 family members.

2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDESupplier

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