An anticancer compound
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CGK733

Item No. 16242

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α-phenyl-N-[2,2,2-trichloro-1-[[[(4-fluoro-3-nitrophenyl)amino]thioxomethyl]amino]ethyl]-benzeneacetamide
CAS Number
905973-89-9
Synonyms
  • ATM/ATR Kinase Inhibitor
Molecular Formula
C23H18Cl3FN4O3S
Formula Weight
555.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 50 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
240, 275 nm
SMILES
FC1=C([N+]([O-])=O)C=C(NC(NC(C(Cl)(Cl)Cl)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=S)C=C1
InChi Code
InChI=1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35)
InChi Key
HLCDNLNLQNYZTK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $63

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    10 mg

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    25 mg

    $168

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    50 mg

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    Product Description

    CGK733 is an anticancer compound that was originally identified as an inhibitor of ataxia-telangiectasia mutated kinase (ATM) and ataxia-telangiectasia and Rad3-related kinase (ATR) in a study that has since been retracted.1,2 It inhibits irradiation-induced activation of ATM in a reporter assay using HEK293 cells when used at a concentration of 10 µM but does not inhibit irradiation-induced activation of ATM or checkpoint kinase 2 (Chk2) in H460 human lung cancer cells or UV radiation-induced phosphorylation of Chk1 at serine 317 at the same concentration.3,4 It also inhibits ATM activity in a bioluminescence-based reporter D54 glioblastoma mouse xenograft model when administered at a dose of 25 mg/kg.3 CGK733 reduces tumor growth in a CNE-2 nasopharyngeal carcinoma mouse xenograft model.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Won, J., Kim, M., Kim, N., et al. Small molecule-based reversible reprogramming of cellular lifespan. Nat. Chem. Biol. 2(7), 369-374 (2006).

    2. Won, J., Kim, M., Kim, N., et al. Retraction: Small molecule-based reversible reprogramming of cellular lifespan. Nat. Chem. Biol. 4(7), 431 (2008).

    3. Williams, T.M., Nyati, S., Ross, B.D., et al. Molecular imaging of the ATM kinase activity. Int. J. Radiat. Oncol. Biol. Phys. 86(5), 969-977 (2013).

    4. Choi, S., Toledo, L.I., Fernandez-Capetillo, O., et al. CGK733 does not inhibit ATM or ATR kinase activity in H460 human lung cancer cells. DNA Repair (Amst) 10(10), 1000-1001 (2011).

    5. Wang, M., Liu, G., Shan, G.-P., et al. In vivo and in vitro effects of ATM/ATR signaling pathway on proliferation, apoptosis, and radiosensitivity of nasopharyngeal carcinoma cells. Cancer Biother. Radiopharm. 32(6), 193-203 (2017).