R&D Systems Inc. Tocris Bioscience Boston Biochem

CGK 733

Cat. No. 2639

CGK 733 C23H18Cl3FN4O3S [905973-89-9]

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Chemical Name: α-Phenyl-N-[2,2,2-trichloro-1-[[[(4-fluoro-3-nitrophenyl)amino]thioxomethyl]amino]ethyl]benzeneacetamide

Biological Activity

Originally defined as a selective inhibitor of ATR and ATM kinases. Induces cell death in prematurely senescent breast cancer cells. Decreases p21CIP1 levels in premature senescent MCF-7 and HCT-116 cells; also exhibits antiproliferative activity in a range of cancer cell lines. Blocks camptothecin-induced p53 phosphorylation and protects cells from camptothecin-induced apoptosis.

Technical Data

M.Wt:
555.84
Formula:
C23H18Cl3FN4O3S
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
905973-89-9

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Crescenzi et al (2008) Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: Implications for chemotherapy. Clin.Cancer Res. 14 1877. PMID: 18347191.

Cruet-Hennequart et al (2008) Enhanced DNA-PK-mediated RPA2 hyperphosphorylation in DNA polymerase η-deficient human cells treated with cisplatin and oxaliplatin. DNA Repair 7 582. PMID: 18289945.

Goldstein et al (2008) Apoptotic death induced by the cyclophosphamide analogue mafosfamide in human lymphoblastoid cells: Contribution of DNA replication, transcription inhibition and Chk/p53 signaling. Toxicol.Appl.Pharmacol. 229 20. PMID: 18289623.

Won et al (2008) Retraction: small molecule-based reversible reprogramming of cellular lifespan. Nat.Chem.Biol. 4 431. PMID: 18560433.

Alao and Sunnerhagen (2009) The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Radiat.Oncol. 10 4. PMID: 19903334.

Bhattacharya et al (2009) Role of polyamines in p53-dependent apoptosis of intestinal epithelial cells. Cell Signal. 21 509. PMID: 19136059.

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Keywords: CGK 733, supplier, CGK733, p21, antiproliferative, p53

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