1. Apoptosis
  2. Apoptosis
  3. TREM2-IN-1

TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206+ and CX3CR1+ immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells.

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TREM2-IN-1 Chemical Structure

TREM2-IN-1 Chemical Structure

CAS No. : 2000236-36-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206+ and CX3CR1+ immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells[1].

IC50 & Target

TREM2[1]

In Vitro

TREM2-IN-1 (0.8 μM, 72 h) inhibits the prophase of DNA synthesis (G1 phase) and has potent proapoptotic ability in HCT-116 cells[1].
TREM2-IN-1 (1 μM, 24 h) remarkably inhibits the expression of TREM2 in the THP-1-derived macrophages[1].

IC50 (μM) of TREM2-IN-1 at 72 h against different cell lines[1]

Complex HCT-116 HepG2 PANC-1 U87-MG HK-2
TREM2-IN-1 0.84 7.32 5.26 22.23 16.29

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.8 μM
Incubation Time: 72 h
Result: Increased the cells in the G1 phase from 24.81% to 48.96% in HCT-116 cells.

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.8 μM
Incubation Time: 72 h
Result: Induced 5.17% and 30.9% of HCT-116 cells to enter the early and late apoptosis respectively at 0.8 μM.
In Vivo

TREM2-IN-1 (1.5 mg Pt per kg, treat, a single dose for 15 days) effectively inhibits the growth of tumor with low general toxicity in C57BL/6 mice models bearing MC38 murine colorectal cancer[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice models bearing MC38 murine colorectal cancer[2]
Dosage: 1.5 mg Pt per kg
Administration: treat, a single dose for 15 days
Result: Effectively suppressed the tumor growth to the volume of 185.75 mm3 in C57BL/6 mice models bearing MC38 murine colorectal cancer.
Molecular Weight

1164.12

Formula

C46H68N2O20Pt

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@@H]1[C@H](C)[C@@](CC[C@@H](C)[C@]2([H])CC[C@](OO3)(C)O4)([H])[C@@]23[C@]4([H])O1)CCC(O[Pt]5(OC6=O)(OC6=O)(OC(CCC(O[C@@H]7[C@H](C)[C@@](CC[C@@H](C)[C@]8([H])CC[C@]9(C)O%10)([H])[C@@]8(OO9)[C@]%10([H])O7)=O)=O)[NH2][C@H](CCCC%11)[C@@H]%11[NH2]5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (85.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8590 mL 4.2951 mL 8.5902 mL
5 mM 0.1718 mL 0.8590 mL 1.7180 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8590 mL 4.2951 mL 8.5902 mL 21.4754 mL
5 mM 0.1718 mL 0.8590 mL 1.7180 mL 4.2951 mL
10 mM 0.0859 mL 0.4295 mL 0.8590 mL 2.1475 mL
15 mM 0.0573 mL 0.2863 mL 0.5727 mL 1.4317 mL
20 mM 0.0430 mL 0.2148 mL 0.4295 mL 1.0738 mL
25 mM 0.0344 mL 0.1718 mL 0.3436 mL 0.8590 mL
30 mM 0.0286 mL 0.1432 mL 0.2863 mL 0.7158 mL
40 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5369 mL
50 mM 0.0172 mL 0.0859 mL 0.1718 mL 0.4295 mL
60 mM 0.0143 mL 0.0716 mL 0.1432 mL 0.3579 mL
80 mM 0.0107 mL 0.0537 mL 0.1074 mL 0.2684 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TREM2-IN-1
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HY-160421
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