CGK 733

Catalog No.S7136

For research use only.

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

CGK 733 Chemical Structure

CAS No. 905973-89-9

Selleck's CGK 733 has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

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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 Research:[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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 555.84
Formula

C23H18Cl3FN4O3S

CAS No. 905973-89-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC3=CC(=C(C=C3)F)[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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

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