CGK 733

Catalog No.S7136 Batch:S713601

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Technical Data

Formula

C23H18Cl3FN4O3S
Molecular Weight 555.84 CAS No. 905973-89-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (179.9 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
Targets
ATM [1] ATR [1]
200 nM 200 nM
In vitro CGK733 is able to confer robust growth to senescent cells that have ceased proliferation. Senescence-associated β-galactosidase (SA–β-gal) activity disappears in CGK733-treated cells. CGK733 shows greater potency in inhibiting ATM/ATR than LY294002 (IC50 , ~5 μM for ATM and ATR), a pan-inhibitor of PI3K and PIKKs. [1] CGK733 (30 μM) treated for 24h causes ~60% cell death in senescent MCF-7 cells. [2] CGK733 (20 μM) induces the loss of cyclin D1 via the ubiquitin- dependent proteasomal degradation pathway in MCF-7 and T47D breast cancer cell lines. CGK733 at concentrations ranging from 0.6- 40 μM, inhibits proliferation of MCF-7 and T47D estrogen receptor (ER) positive breast cancer cells, MDA-MB436 ER negative breast cancer cells, LnCap pros-tate cancer cells and HCT116 colon cancer cells. Furthermore, CGK733 also suppresses proliferation of non- transformed mouse BALB/c 3T3 embryonic fibroblast cells. The CGK733-mediated inhibition of proliferation is dose dependent and significant at doses as low as 2.5 μM. [3]

Protocol (from reference)

Cell Assay:[3]
  • Cell lines

    Human breast cancers cell line MCF-7

  • Concentrations

    ~20 μM

  • Incubation Time

    2 days

  • Method

    Cells are seeded in 96-well plates at a predetermined, optimal cell density to ensure exponential growth for duration of the assay. After a 24 h preincubation, growth medium is replaced with experimental medium containing the appropriate drug concentrations or 0.1% (v/v) vehicle control. After a 48 h incubation, cell proliferation is estimated using the sulforhodamine B colorimetric assay.

Customer Product Validation

Data from [Data independently produced by , , Molecules and Cells， 2016， 39(12): 869-876.]

Selleck's CGK 733 has been cited by 5 publications

p53-driven replication stress in nucleoli of malignant epithelial ovarian cancer [ Exp Cell Res, 2022, S0014-4827(22)00218-X] PubMed: 35644414
Selenomethionine protects hematopoietic stem/progenitor cells against cobalt nanoparticles by stimulating antioxidant actions and DNA repair functions [ Aging (Albany NY), 2021, 13(8):11705-11726] PubMed: 33875618
Involvement of Host ATR-CHK1 Pathway in Hepatitis B Virus Covalently Closed Circular DNA Formation. [ mBio, 2020, 11(1)] PubMed: 32071277
Cantharidin Overcomes Imatinib Resistance by Depleting BCR-ABL in Chronic Myeloid Leukemia. [Sun X, et al. Mol Cells, 2016, 39(12):869-876] PubMed: 27989101
URI1 amplification in uterine carcinosarcoma associates with chemo-resistance and poor prognosis [ Am J Cancer Res, 2015, 5(7):2320-9] PubMed: 26328264

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.