CGK 733

貨號 Cat. No.
S7136
規格 Size
10mg、50mg
品牌 Brand
Selleckchem

Description

 



CGK 733
Catalog No.S7136

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


















Size Price Stock Quantity  
















10mg USD 185 In stock  
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50mg USD 592 In stock  
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw


Biological Activity







































Description CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
Targets ATM ATR        
IC50 200 nM 200 nM [1]        
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]
In vivo  
Features  

Protocol(Only for 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.

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References


Chemical Information


Download CGK 733 SDF


 

















Molecular Weight (MW) 555.84
Formula

C23H18Cl3FN4O3S


CAS No. 905973-89-9















Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A

 





















Solubility (25°C) * In vitro DMSO 100 mg/mL (179 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <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.


 








Chemical Name Benzeneacetamide, α-phenyl-N-[2,2,2-trichloro-1-[[[(4-fluoro-3-nitrophenyl)amino]thioxomethyl]amino]ethyl]-

 

Preparing Stock Solutions



















Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.55584 5.5584 11.1168 16.6752


 


 


 


 


 


 


 

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