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Fig. 1 · Structure
Cat. No.
A10922
CAS No.
677297-51-7
Formula
C18H14N6O2
Mol. Weight
346.3

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TG100-115

Cat. No. A10922 CAS 677297-51-7

PI3K Inhibitor

TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).

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Biological Activity

Target & Activity

Target Activity Value
PI3Kγ 83 nM
PI3Kδ 235 nM
PI3Kβ 1.2 μM
PI3Kα 1.3 μM

In Vitro Studies

In primary human neutrophils from healthy donors, TG100-115 did not affect TRPM7 channel activity in patch-clamp recordings. TG100-115-treated BMDMs engulfed a lower percentage of dying heat-treated GFP-transfected Hepa1-6 cells compared with DMSO-treated BMDMs. In human neutrophils, TG100-115 significantly reduced CXCL8-triggered chemotaxis compared with the dissolvent control. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Channel Activity in Primary Human Neutrophils

Cell-based study · primary human neutrophils isolated from whole blood of healthy donors [1]

Primary human neutrophils isolated from healthy donor whole blood were preincubated with TG100-115 at 20 µM for 30 min. TG100-115 did not affect TRPM7 channel activity in patch-clamp recordings.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
TRPM7 current densitiesReported result TG100-115 (20 µM, 30 min pre-incubation), did not affect channel activity in our patch-clamp recordings[1]

Literature-Reported Treatment Conditions

Treatment concentration
20 µM
Exposure duration
at least 30 min prior to electrophysiological recordings
Method
added to the bath solution
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: TG100-115

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Material and Methods > Electrophysiology (S26); Results > TRPM7 Is Essential for Human Neutrophil Chemotaxis and ROS Production (S53, S56); Figure 1 legend (S118)

TRPM7 current densities: TRPM7 current densities; comparator: without (Ctrl, black circles, n = 6) — Results > TRPM7 Is Essential for Human Neutrophil Chemotaxis and ROS Production (S56); Figure 1 legend (S118)

Engulfment of Dying Cells by Macrophages

Cell-based study · BMDMs; n = 3 [2]

BMDMs were pretreated with TG100-115 and assessed for phagocytosis of heat-treated GFP-transfected Hepa1-6 cells. TG100-115-treated BMDMs engulfed a lower percentage of dying cells than DMSO-treated BMDMs.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
flow cytometry plots illustrating macrophages treated with TG100‐115 phagocytosis of heat‐treated GFP‐transfected Hepa1‐6 cellsReported result TG100‐115‐treated BMDMs engulfed a lower percentage of dying cells compared with DMSO‐treated BMDMs[2]

Literature-Reported Treatment Conditions

Method
pretreated
Vehicle
DMSO
Co-treatment
Other interventions in this design: heat‐treated GFP‐transfected Hepa1‐6 cells. Compound effect isolated by the comparison: compared with DMSO‐treated BMDMs.
Reported limits
Not stated in the sentences used: dose, schedule.
Methods and source locations

Compound reported in the paper: TG100-115

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Macrophages Undergoing LAP Activate the PI3Kγ/AKT Pathway (S93); Figure 5 legend (S201)

flow cytometry plots illustrating macrophages treated with TG100‐115 phagocytosis of heat‐treated GFP‐transfected Hepa1‐6 cells: flow cytometry plots illustrating macrophages treated with TG100‐115 phagocytosis of heat‐treated GFP‐transfected Hepa1‐6 cells; comparator: DMSO‐treated BMDMs — Results > Macrophages Undergoing LAP Activate the PI3Kγ/AKT Pathway (S93); Figure 5 legend (S201)

Chemokine-Triggered Neutrophil Chemotaxis

Cell-based study · Human neutrophils [1]

Human neutrophils were incubated with TG100-115 at 20 µM for 30 min before CXCL8 or saline exposure. In a transwell assay, TG100-115 significantly reduced CXCL8-triggered chemotaxis compared with the dissolvent control.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
neutrophil chemotaxis toward a CXCL8 gradient (10 nM) in a transwell assayReported result TG100-115 (20 µM, 30 min pre-incubation): a significant reduction in neutrophil CXCL8-triggered chemotaxis[1]

Literature-Reported Treatment Conditions

Treatment concentration
20 µM
Exposure duration
for 30 min prior to CXCL8 or saline (Ctrl) exposure
Method
incubated
Vehicle
DMSO
Co-treatment
Other interventions in this design: CXCL8 10nM. Compound effect isolated by the comparison: dissolvent (Ctrl, black).
Methods and source locations

Compound reported in the paper: TG100-115

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Material and Methods > Transwell Assay (S27, S28, S32, S33); Results > TRPM7 Is Essential for Human Neutrophil Chemotaxis and ROS Production (S59); Figure 1 legend (S123, S124)

neutrophil chemotaxis toward a CXCL8 gradient (10 nM) in a transwell assay: neutrophil chemotaxis toward a CXCL8 gradient (10 nM) in a transwell assay; comparator: DMSO (Ctrl.) — Results > TRPM7 Is Essential for Human Neutrophil Chemotaxis and ROS Production (S59); Figure 1 legend (S123)

In Vivo Studies

TG100-115 solution was administered intravenously at 30 mg/kg in a Hep-3B-xenografted nude mouse model, with normal saline as the comparator. Tumor weight in the TG100-115 solution group was 2.72 ± 0.31 g. [3]

Tumor Weight in a Nude Mouse Xenograft Model

Animal study · Hep-3B-xenografted nude mouse model; n = 6 [3]

In the Hep-3B-xenografted nude mouse model, TG100-115 solution was administered intravenously at 30 mg/kg, with normal saline as the comparator. Tumor weight in the TG100-115 solution group was 2.72 ± 0.31 g.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tumor weight (g)Tumor weight TG100-115 solution, 30 mg/kg: 2.72 ± 0.31 g[3]

Conditions shared by the study groups

Route
intravenous administration
Treatment course
twice a week for 4 weeks; sacrificed on day 28
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
TG100-115 30 mg/kgNormal salineTG100-115 solution, 30 mg/kg: 2.72 ± 0.31 g[3]
TG100-115 30 mg/kg
Model: Hep-3B-xenografted nude mouse model; n = 6
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: TG100-115

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and methods > In vivo pharmacodynamic evaluations (S60, S61, S62, S63, S64, S65); Figure 3. legend (S75); Table 2. (T2.h1, T2.r1, T2.r2)

Tumor weight (g): Tumor weight (g); comparator: Normal saline — Table 2. (T2.h1, T2.r2)

TG100-115 30 mg/kg · Materials and methods > In vivo pharmacodynamic evaluations (S63, S64, S65); Figure 3. legend (S75); Table 2. (T2.h1, T2.r2)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 677297-51-7
Applications PI3K Inhibitor
Formula C18H14N6O2
Molecular Weight 346.3
SMILES
C1=CC(=CC(=C1)O)C2=NC3=C(N=C2C4=CC(=CC=C4)O)N=C(N=C3N)N

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 8 mg/mL (23.09 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
0.3 mg/mL
Vehicle
5% DMSO+30% PEG 300+ddH2O

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Nadolni W, Immler R, Hoelting K, et al. TRPM7 Kinase Is Essential for Neutrophil Recruitment and Function via Regulation of Akt/mTOR Signaling. Front Immunol (2020). PMID: 33658993 DOI: 10.3389/fimmu.2020.606893 Source material
  2. [2] Liu X, Zhang W, Xu Y, et al. Targeting PI3Kγ/AKT Pathway Remodels LC3-Associated Phagocytosis Induced Immunosuppression After Radiofrequency Ablation. Adv Sci (Weinh) (2022). PMID: 35037422 DOI: 10.1002/advs.202102182 Source material
  3. [3] Li G, Zhao L. Sorafenib-loaded hydroxyethyl starch-TG100-115 micelles for the treatment of liver cancer based on synergistic treatment. Drug Deliv (2019). PMID: 31357893 DOI: 10.1080/10717544.2019.1642418 Source material

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