CGK 733

Catalog No.S7136

CGK 733 Chemical Structure

Molecular Weight(MW): 555.84

CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.

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1 Customer Review

  • K562 and K562R cells were pre-treated for 1 h with CGK733 (5 μM), then treated with CTD (10 μM) for 24 h, and protein levels of cleaved PARP, Mcl-1, and phosphorylated H3 were determined by Western blotting. GAPDH served as a normal control.

    Molecules and Cells, 2016, 39(12): 869-876.. CGK 733 purchased from Selleck.

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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

Cell Research:[3]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (179.9 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 555.84
Formula

C23H18Cl3FN4O3S

CAS No. 905973-89-9
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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ATM/ATR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID