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Chemical Structure| 677297-51-7 Chemical Structure| 677297-51-7

Structure of TG100-115
CAS No.: 677297-51-7

Chemical Structure| 677297-51-7

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TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β.

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Product Details of TG100-115

CAS No. :677297-51-7
Formula : C18H14N6O2
M.W : 346.34
SMILES Code : NC1=C2N=C(C3=CC(O)=CC=C3)C(C4=CC(O)=CC=C4)=NC2=NC(N)=N1
MDL No. :MFCD16038873

Safety of TG100-115

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

Related Pathways of TG100-115

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:83 nM

  • p110β

    PI3Kβ, IC50:1.2 μM

  • p110α

    PI3Kα, IC50:1.3 μM

  • p110δ

    PI3Kδ, IC50:235 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human umbilical vein EC 10 μM 15 minutes Detect VEGF-stimulated VE-cadherin and ERK1/2 phosphorylation, TG100-115 blocked VE-cadherin phosphorylation but did not affect ERK1/2 phosphorylation PMC1702529
Human umbilical vein EC 10 μM 24-72 hours Assess cell proliferation, TG100-115 did not affect endothelial cell proliferation at concentrations up to 10 μM PMC1702529
Murine bone marrow-derived neutrophils 20 µM 30 minutes To evaluate the effect of TRPM7 kinase activity on murine neutrophil chemotaxis. Results showed that TG100-115 significantly reduced neutrophil migration toward a CXCL1 gradient. PMC7917126
Human neutrophils 20 µM 30 minutes To evaluate the effect of TRPM7 kinase activity on human neutrophil chemotaxis and ROS production. Results showed that TG100-115 significantly reduced neutrophil migration toward a CXCL8 gradient and decreased LPS-induced ROS production. PMC7917126
Hep-3B 5.0, 25.0, 100.0, 250.0 mg/mL 48 and 72 hours Evaluate the cytotoxicity of HES-TG100-115-CDM-PEG micelles on Hep-3B cells. Results showed that HES-CHO exhibited good safety and biocompatibility with no significant inhibitory effects on Hep-3B cells at all concentrations. PMC6711177

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Myocardial ischemia/reperfusion injury model Intravenous injection 0.5 mg/kg Single dose Evaluate cardioprotective effects, TG100-115 reduced infarct size by ~40% when administered up to 3 hours post-reperfusion and improved myocardial function PMC1702529
Nude mice Hep-3B xenograft model Intravenous injection 30 mg/kg (TG100-115) and 20 mg/kg (sorafenib) Twice a week for 4 weeks Evaluate the anti-tumor activity and safety of HES-TG100-115-CDM-PEG micelles in the Hep-3B xenograft model. Results showed that the micelles group exhibited better anti-tumor effects than the free drug groups, with a tumor inhibition rate of 88.70%. PMC6711177

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00103350 Myocardial Infarction PHASE1|PHASE2 COMPLETED 2025-01-08 David Holmes, MD, Rochester, M... More >>innesota, 55905, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.44mL

2.89mL

1.44mL

28.87mL

5.77mL

2.89mL

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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