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Chemical Structure| 164658-13-3 Chemical Structure| 164658-13-3

Structure of CGP60474
CAS No.: 164658-13-3

Chemical Structure| 164658-13-3

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CGP60474 is a promising inhibitor of PKC with a high degree of selectivity versus other serine/threonine and tyrosine kinases and show competitive kinetics relative to ATP.

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Product Details of CGP60474

CAS No. :164658-13-3
Formula : C18H18ClN5O
M.W : 355.82
SMILES Code : ClC1=CC(NC2=NC=CC(C3=CC=NC(NCCCO)=C3)=N2)=CC=C1
MDL No. :MFCD00938945
InChI Key :IYNDTACKOAXKBJ-UHFFFAOYSA-N
Pubchem ID :644215

Safety of CGP60474

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of CGP60474

epigenetics
GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
EHE17 cells 500 nM 16 hours CGP60474, by inhibiting CDK9, reduced TC nuclear localization and promoted its degradation, significantly suppressing TC-dependent transcription and cell viability. PMC11398983
EHE6 cells 500 nM 16 hours CGP60474 significantly reduced the viability of EHE6 cells. PMC11398983
EHE26 cells 500 nM 16 hours CGP60474 significantly reduced the viability of EHE26 cells. PMC11398983
Schistosoma mansoni schistosomula 10 µM 72 h To evaluate the anti-schistosomal activity of CGP60474 on Schistosoma mansoni schistosomula, results showed that CGP60474 exhibited significant anti-schistosomal activity at 10 µM concentration. PMC10220823
J774.1 cells 100 ng/ml LPS 24 hours CGP-60474 inhibited IL-6 secretion in LPS-stimulated J774.1 cells in a concentration-dependent manner. PMC6175892
Bone marrow-derived macrophages (BMDMs) 100 ng/ml LPS 24 hours CGP-60474 inhibited IL-6 secretion in LPS-stimulated BMDMs in a concentration-dependent manner. PMC6175892
BJ fibroblasts 1 µM 24 hours To assess the effect of CGP60474 on cell viability and collagen secretion, results showed that CGP60474 significantly inhibited collagen I secretion with minimal effect on cell viability. PMC10831310
KF1, KF4, KF5, KF6 1 µM 24 hours To assess the effect of CGP60474 on cell viability and collagen secretion, results showed that CGP60474 significantly inhibited collagen I secretion with minimal effect on cell viability. PMC10831310

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice EHE17 cell xenograft model Intraperitoneal injection 1% DFMO and 2.5 mg/kg/day AMXT 1501 Continuous for 4 weeks CGP60474 was not used in in vivo experiments, dinaciclib significantly reduced the area of lung metastatic lesions in the EHE17 cell xenograft model. PMC11398983
Mus musculus Schistosoma mansoni infection model in vitro culture 1μM daily for 14 days To evaluate the activity of CGP60474 on adult Schistosoma mansoni, results showed that CGP60474 completely inhibited worm movement within the first 24 h of treatment. PMC10220823
Mice LPS-induced endotoxemia model Intraperitoneal injection 37.5mg/kg, 75mg/kg, 112.5mg/kg Every 8 hours, three times CGP-60474 improved survival rate and reduced plasma IL-6 levels in LPS-induced endotoxemia mouse model. PMC6175892

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.05mL

2.81mL

1.41mL

28.10mL

5.62mL

2.81mL

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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