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Chemical Structure| 1159824-67-5 Chemical Structure| 1159824-67-5

Structure of CZC24832
CAS No.: 1159824-67-5

Chemical Structure| 1159824-67-5

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CZC-24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and > 100-fold selectivity over PI3Kα and PI3Kδ.

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Product Details of CZC24832

CAS No. :1159824-67-5
Formula : C15H17FN6O2S
M.W : 364.40
SMILES Code : O=S(C1=CC(C2=CN3C(C(F)=C2)=NC(N)=N3)=CN=C1)(NC(C)(C)C)=O
MDL No. :MFCD22417090
InChI Key :RXRZPHQBTHQXSV-UHFFFAOYSA-N
Pubchem ID :42623951

Safety of CZC24832

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P280-P305+P351+P338-P337+P313

Related Pathways of CZC24832

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:27 nM

  • p110β

    PI3Kβ, IC50:1.1 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Ramos cells 2 μM 1 hour To assess the effect of PI3Kγ inhibition on Ramos cell migration, results showed that PI3Kγ inhibition significantly reduced the migration of Ramos cells. PMC6127087
CLL cells 2 μM 1 hour To assess the effect of PI3Kγ inhibition on CLL cell migration, results showed that PI3Kγ inhibition significantly reduced the migration of CLL cells. PMC6127087
JVM3 cells 2 μM 1 hour To assess the effect of PI3Kγ inhibition on JVM3 cell migration, results showed that PI3Kγ inhibition significantly reduced the migration of JVM3 cells. PMC6127087
SJCRH30 cells 0–20 μM 72 hours Evaluate the effect of CZC24832 on SJCRH30 cell proliferation, results showed no significant effect on SJCRH30 cell viability PMC9104989
A204 cells 0–20 μM 72 hours Evaluate the effect of CZC24832 on A204 cell proliferation, results showed effect on A204 cell viability PMC9104989
RD cells 0–20 μM 72 hours Evaluate the effect of CZC24832 on RD cell proliferation, results showed no significant effect on RD cell viability PMC9104989

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Cecal ligation and puncture (CLP)-induced septic cardiomyopathy model Oral gavage 10 mg/kg/day Once daily, starting one day before CLP surgery until the end of observation To evaluate the protective effect of CZC24832 on septic cardiomyopathy, results showed that CZC24832 significantly reduced animal lethality, improved cardiac function, and reduced inflammatory cell infiltration PMC9198581

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL

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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