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Chemical Structure| 905973-89-9 Chemical Structure| 905973-89-9

Structure of CGK733
CAS No.: 905973-89-9

Chemical Structure| 905973-89-9

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CGK 733 is an inhibitor of ATM and ATR with IC50 of ~200 nM, also induces cell death in prematurely senescent breast cancer cells.

Synonyms: ATM/ATR Kinase Inhibitor

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Product Details of CGK733

CAS No. :905973-89-9
Formula : C23H18Cl3FN4O3S
M.W : 555.84
SMILES Code : O=C(NC(NC(NC1=CC=C(F)C([N+]([O-])=O)=C1)=S)C(Cl)(Cl)Cl)C(C2=CC=CC=C2)C3=CC=CC=C3
Synonyms :
ATM/ATR Kinase Inhibitor
MDL No. :MFCD09038682
InChI Key :HLCDNLNLQNYZTK-UHFFFAOYSA-N
Pubchem ID :6605258

Safety of CGK733

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CGK733

DNA
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • ATM

    ATM, IC50:200 nM

  • ATR

    ATR, IC50:200 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
BALB/c 3T3 mouse embryonic fibroblasts 2.5-20 μM 48 h Inhibited cell proliferation PMC2777912
HCT116 colon cancer cells 2.5-20 μM 48 h Inhibited cell proliferation PMC2777912
CaSki cells 50 nM 24 h Inhibited ATM activity, reversed HDAB-induced S phase arrest and promoted apoptosis PMC4455115
HeLa cells 50 nM 24 h Inhibited ATM activity, reversed HDAB-induced S phase arrest and promoted apoptosis PMC4455115
Bone marrow-derived macrophages (BMMs) 1-6 μM 96 h, 48 h, 7 days Evaluate cytotoxicity, apoptosis, and inhibitory effects of CGK733 on osteoclast differentiation. Results showed CGK733 had no cytotoxicity at 1-6 μM, did not induce apoptosis, and dose-dependently inhibited RANKL-induced osteoclast differentiation, with optimal effect at 6 μM. PMC10504545
LNCaP prostate cancer cells 10 μM 6 h Induced decline in cyclin D1 protein levels via ubiquitin-26S proteasome pathway PMC2777912
T47D breast cancer cells 5-20 μM 6 h Induced decline in cyclin D1 protein levels via ubiquitin-26S proteasome pathway PMC2777912
MCF-7 breast cancer cells 10 μM 2-6 h Induced decline in cyclin D1 protein levels via ubiquitin-26S proteasome pathway PMC2777912

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J female mice Ovariectomy (OVX)-induced osteoporosis model Intraperitoneal injection 3 mg/kg or 6 mg/kg Every other day for 6 weeks Evaluate therapeutic effects of CGK733 on OVX-induced bone loss. Results showed CGK733 (especially 6 mg/kg) significantly ameliorated OVX-induced bone microstructure deterioration, reduced osteoclast numbers, increased trabecular bone volume/tissue volume (BV/TV), trabecular number (Tb.N) and thickness (Tb.Th), decreased trabecular separation (Tb.Sp), and showed no toxicity to heart, liver, or kidney. PMC10504545

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

17.99mL

3.60mL

1.80mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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