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Chemical Structure| 648449-76-7 Chemical Structure| 648449-76-7

Structure of AS-604850
CAS No.: 648449-76-7

Chemical Structure| 648449-76-7

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AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, showing over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and being 18-fold selective for PI3Kγ than PI3Kα.

Synonyms: AS-604850

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Product Details of AS-604850

CAS No. :648449-76-7
Formula : C11H5F2NO4S
M.W : 285.22
SMILES Code : O=C(NC/1=O)SC1=C\C2=CC=C(OC(F)(F)O3)C3=C2
Synonyms :
AS-604850

Safety of AS-604850

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317
Precautionary Statements:P280

Related Pathways of AS-604850

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:0.25 μM

  • p110α

    PI3Kα, IC50:4.5 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Raji cells 6.7 μM 72 h AS604850 had weak inhibitory effect on Raji cell proliferation PMC4003165
PC-3 cells 6.7 μM 72 h AS604850 had weak inhibitory effect on PC-3 cell proliferation PMC4003165
Neutrophils 1,000, 100, 10, 1, 0.1 nM Evaluate the effect of AS-604850 on IL-8-induced neutrophil chemotaxis PMC8452940
Neutrophils 5 µM 5 min Evaluate the effect of AS-604850 on kinase activity in IC-activated neutrophils PMC8452940
Neutrophils 1,000, 100, 10, 1, 0.1 nM Evaluate the effect of AS-604850 on IC-induced ROS release from neutrophils PMC8452940
INS-1 832/13 cells 1 μM Overnight We find that p110 γ inhibition severely impairs glucose-stimulated Rac1 activation, without affecting total Rac1 levels. PMC4231687
Human islets 1 μM Overnight The secretory response to GIP was also blunted by p110 γ inhibition in islets from six human donors. PMC4231687
Mouse islets 1 μM Overnight Inhibition of PI3K γ blunted the exocytotic and insulinotropic response to GIP receptor activation, whereas responses to the glucagon-like peptide-1 or the glucagon-like peptide-1 receptor agonist exendin-4 were unchanged. PMC4231687
Huh7-Ntcp cells 2.5 μM 30 min Inhibition of p110 γ activity significantly reduced hydrophobic bile salt-induced apoptosis PMC2949543
HepG2-Ntcp cells 2.5 μM 30 min Inhibition of p110 γ activity significantly reduced hydrophobic bile salt-induced apoptosis PMC2949543
Rat hepatocytes 2.5 μM 30 min Inhibition of p110 γ activity significantly reduced GCDC-induced Akt phosphorylation and apoptosis PMC2949543
Rh30-Myr-p110γ cells 6.7 μM 1 h AS604850 significantly inhibited Akt phosphorylation in Rh30-Myr-p110γ cells, showing selective inhibition against PI3Kγ PMC4003165

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse Langendorff-perfused heart model Perfusion 1 μM Administered prior to ischemia AS-604850 inhibited PI3K-IB activity, blocked IPC-induced protection, but did not affect OPC protection. PMC4827870

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.51mL

0.70mL

0.35mL

17.53mL

3.51mL

1.75mL

35.06mL

7.01mL

3.51mL

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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