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Chemical Structure| 371242-69-2 Chemical Structure| 371242-69-2

Structure of IC-87114
CAS No.: 371242-69-2

Chemical Structure| 371242-69-2

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IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay.

4.5 *For Research Use Only !

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Product Details of IC-87114

CAS No. :371242-69-2
Formula : C22H19N7O
M.W : 397.43
SMILES Code : O=C1N(C2=CC=CC=C2C)C(CN3C=NC4=C(N)N=CN=C34)=NC5=C1C(C)=CC=C5
MDL No. :MFCD09970845

Safety of IC-87114

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

Related Pathways of IC-87114

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:29 μM

  • p110δ

    PI3Kδ, IC50:0.5 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
murine macrophages 1 µM 2 hours inhibited AKT phosphorylation, reduced viral particle attachment PMC7210704
CD8+ OT1 T cells 5 μM 48 hours To study the effect of p110 δ on cytokine production after TCR stimulation, results showed that IC significantly inhibited IFN γ production. PMC3593196
CD4+ OT2 T cells 5 μM 48 hours To study the effect of p110 δ on cytokine production after TCR stimulation, results showed that IC significantly inhibited IFN γ production. PMC3593196
CD62L+ CD4+ T cells 1 μM 48 hours To study the effect of p110 δ on the activation of naïve and effector/memory CD4+ T cells, results showed that IC significantly inhibited IFN γ production. PMC3593196
CD62L− CD4+ T cells 1 μM 48 hours To study the effect of p110 δ on the activation of naïve and effector/memory CD4+ T cells, results showed that IC significantly inhibited IFN γ production. PMC3593196
Murine tracheal epithelial cells (TECs) 10 μmol/L 2 hours To verify the role of PI3K-δ in the regulation of ER stress in Af-stimulated primary cultured TECs, IC87114 significantly reduced Af-induced increases in GRP78 and CHOP. PMC4717427

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Cigarette smoke exposure model Oral 80 mg/kg/day Once daily, continued until the end of the experiment To evaluate the effect of IC-87114 on reversing corticosteroid insensitivity in cigarette smoke-exposed mice, results showed that IC-87114 combined with dexamethasone significantly inhibited alveolar macrophage and neutrophil accumulation PMC2970861
mice CT26 colorectal cancer model oral 80 mg/kg/day Once daily for 2 months enhanced tumor localization of virus, improved anti-tumor efficacy PMC7210704
mice WT B6 mice oral 20 mg/kg Twice daily for 3 days To study the effect of IC on T cell-dependent cytokine production, results showed that IC significantly reduced IL2, IL4, IL17, IFN γ, and TNF α levels in the serum. PMC3593196
C57BL/6 mice Af-induced allergic lung inflammation model Intratracheal instillation 30 mg/kg single dose To examine the effects of IC87114 on Af-induced allergic lung inflammation, IC87114 significantly reduced Af-induced increases in ER stress markers, UPR-related proteins, inflammatory cell infiltration, and airway hyperresponsiveness. PMC4717427
C57BL/6 mice OVA/LPS-induced asthma model Intratracheal administration 100 mg/kg Once daily, continuous treatment To evaluate the effects of IC87114 on airway inflammation and signaling pathways in the OVA/LPS-induced asthma model. Results showed that IC87114 significantly reduced airway inflammatory cell infiltration, airway hyperresponsiveness, and inhibited PI3K/AKT and NF-κB signaling pathways. PMC5903822
mice amphetamine-induced psychosis model intraperitoneal injection 25 mg/kg 5 days/week for 25 days IC87114 significantly blocked amphetamine-induced hyperlocomotion, suggestive of antipsychotic potential, without affecting spontaneous locomotor activity. PMC3409795
Balb/c nude mice Breast cancer model Oral 15 mg/kg Once daily for 3 weeks IC-87114 significantly inhibited tumour growth and reduced the recruitment of macrophages to tumour sites when administered orally. PMC5992183

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL

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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