| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C23H18Cl3FN4O3S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CGK733 is a potent inhibitor of ATM and ATR, used for cancer research. It is supplied as a white to off-white solid (C23H18Cl3FN4O3S, MW 555.84) at 99.71% purity.
Physical & Chemical Properties
| CAS Number | 905973-89-9 |
|---|---|
| Molecular Formula | C23H18Cl3FN4O3S |
| Molecular Weight | 555.84 g/mol |
| Purity | 99.71% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | FC1=CC=C(NC(NC(C(Cl)(Cl)Cl)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=S)C=C1[N+]([O-])=O |
| Target | ATM, ATR |
| Signaling Pathway | Cell Cycle/DNA Damage; PI3K/Akt/mTOR |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (179.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (179.91 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.50 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Protocol 2
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (3.74 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Data provided by the manufacturer.
In Vitro
Taxol-induced cytotoxicity in HBV-positive HCC cells is enhanced by CGK733 (4.2 ng/μL-12.5 ng/μL). In taxol-treated HBV-positive HCC cells, CGK733 (4.2 ng/μL) speeds up multinucleated cell formation and promotes mitotic exit[1]. Loss of cyclin D1 through the ubiquitin-dependent proteasomal degradation pathway is caused by CGK733 (10 μM) in MCF-7 and T47D breast cancer cell lines. Proliferation of LnCap prostate cancer cells and HCT116 colon cancer cells is inhibited by CGK733 (0.6-40 μM), as is proliferation of MCF-7 and T47D estrogen receptor positive breast cancer cells and of ER negative MDA-MB436 breast cancer cells. Non-transformed mouse BALB/c 3T3 embryonic fibroblast cells also show inhibited proliferation with CGK733. MCF-7 proliferation is also inhibited by CGK733 (10 μM), and pan-caspase inhibition cannot suppress this effect[2]. ATM reporter activity in HEK-293 cells increases 1.6-fold with CGK733 (10 μM)[3].
In Vivo
Compared with control mice, CGK733 (25 mg/kg, i.p.) increases ATM reporter activity (reports inactivation of ATM kinase activity), with 2.4-fold, 3.1-fold, and 1.3-fold changes at 1, 4, and 8 hours, respectively[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[3]
Acclimatize four to six weeks old athymic CD-1 female mice for at least one week before use. Inject 2×106 D54-ATMR cells subcutaneously into each flank. Allow tumors to grow to a size of 100-150 mm3. Inject mice intraperitoneally with vehicle control (DMSO), CGK-733, KU-55933 (25 mg/kg), or irradiate each flank with 5 Gy. Acquire bioluminescence on a Xenogen IVIS Spectrum system after injecting 400 μg/100 μL of D-luciferin at baseline (-3h) and at 1, 4, and 8 hours after drug administration[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
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Selenium-containing ruthenium complex synergizes with natural killer cells to enhance immunotherapy against prostate cancer via activating TRAIL/FasL signaling. Biomaterials 2019 Oct:219:119377. PMID: 31374478
Nano Today. 2025 Jun.
LIG1 Loss in TP53-mutant Triple Negative Breast Cancer Rewires DNA Repair and Confers Sensitivity to PARP-ATR Inhibitor Combinations. Mol Cancer Ther 2026 Jul 15:10.1158/1535-7163.MCT-26-0182. PMID: 42456172
Hexavalent chromium triggers hepatocytes premature senescence via the GATA4/NF-κB signaling pathway mediated by the DNA damage response. Ecotoxicol Environ Saf 2022 May 16;239:113645. PMID: 35588622
Loss of Brcc3 in Zebrafish Embryos Increases Their Susceptibility to DNA Damage Stress. Int J Mol Sci 2024 Nov 11;25(22):12108. PMID: 39596176
Combination of PARP inhibitor and temozolomide to suppress chordoma progression. J Mol Med (Berl) 2019 Aug;97(8):1183-1193.
STM2457 impairs the proliferation of esophageal squamous cell carcinoma by activating DNA damage response through ATM-Chk2 axis. Med Oncol 2025 Feb 22;42(3):82. PMID: 39985567
CGK733 alleviates ovariectomy-induced bone loss through blocking RANKL-mediated Ca2+ oscillations and NF-κB/MAPK signaling pathways. iScience 2023 Aug 29;26(10):107760. PMID: 37720109
