2. Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Glutathione Peroxidase Reactive Oxygen Species (ROS) Apoptosis Ferroptosis PD-1/PD-L1
  4. iMQT_020

iMQT_020 is a selective allosteric SLC1A5_var inhibitor. iMQT_020 disrupts the trimeric assembly of SLC1A5_var, causing metabolic crisis in cancer cells and selectively suppressing their growth. iMQT_020 reduces glutamine anaplerosis and oxidative phosphorylation, resulting in a broad disruption of cancer metabolism. iMQT_020 reduces GSH levels and increases cellular ROS and mitochondrial ROS. iMQT_020 induces apoptosis and ferroptosis. iMQT_020 can epigenetically upregulate PD-L1 expression. iMQT_020 can be used for the study of pancreatic cancer, lung cancer, and colon cancer.

For research use only. We do not sell to patients.

iMQT_020

iMQT_020 Chemical Structure

CAS No. : 2463893-46-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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10 mg In-stock
25 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

iMQT_020 Related Antibodies

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Description

iMQT_020 is a selective allosteric SLC1A5_var inhibitor. iMQT_020 disrupts the trimeric assembly of SLC1A5_var, causing metabolic crisis in cancer cells and selectively suppressing their growth. iMQT_020 reduces glutamine anaplerosis and oxidative phosphorylation, resulting in a broad disruption of cancer metabolism. iMQT_020 reduces GSH levels and increases cellular ROS and mitochondrial ROS. iMQT_020 induces apoptosis and ferroptosis. iMQT_020 can epigenetically upregulate PD-L1 expression. iMQT_020 can be used for the study of pancreatic cancer, lung cancer, and colon cancer[1].

In Vitro

iMQT_020 shows the strongest inhibitory effect on mitochondrial glutamine uptake (IC50 = 6.156 μM) at a concentration of 10 μM[1].
iMQT_020 (0-100 μM) directly binds to SLC1A5_var WT protein (Kd = 4.473 μM), but does not bind to FIL/AAA mutants[1].
iMQT_020 (4 μM) significantly reduces the CD signal of the SLC1A5_var WT protein, indicating a structural change[1].
iMQT_020 (10 μM) reduces glutamine-derived TCA cycle metabolites (such as glutamate, αKG, succinic acid, etc.) and downstream products (such as glutathione, proline) in MIA PaCa-2 cells[1].
iMQT_020 (10 μM, 24 h) reduces GSH levels in MIA PaCa-2 cells and increases cellular ROS and mitochondrial ROS[1].
iMQT_020 (10 μM, 24 h) reduces OCR and ECAR in SLC1A5_var WT-overexpressing MIA PaCa-2 cells, but did not affect FIL/AAA mutants[1].
iMQT_020 (10 μM, 24 h) alters mitochondrial morphology in MIA PaCa-2 cells (reducing fragmentation) and decreases mitochondrial membrane potential (reduced TMRE staining)[1].
iMQT_020 (48 h) selectively inhibits the viability of cancer cells (IC50 5-40 μM) without affecting normal cells[1].
iMQT_020 (10 μM, 24 h) upregulates PD-L1 mRNA and protein expression in human PDAC cell lines (such as SU.86.86, SW1990) and mouse carcinoma cell lines (KPC, LLC, MC-38)[1].

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

iMQT_020 Related Antibodies
In Vivo

iMQT_020 (75 mg/kg, i.p., once daily for 35 days) inhibits tumor growth in mice xenografted with MIA PaCa-2 cells by inducing apoptosis and ferroptosis[1].
iMQT_020 (75 mg/kg, i.p., once daily for 35 days) inhibits tumor growth in a mouse orthotopic transplantation model of MIA PaCa-2 cells[1].
iMQT_020 (75 mg/kg, i.p., once daily for 35 days) inhibits the growth of xenografted tumors of NCI-H1299 human lung cancer cells and COLO 205 human colon cancer cells in mice[1].
iMQT_020 (25 mg/kg, i.p., once daily for 21 days), when used in combination with an anti-PD-L1 antibody (aPD-L1), synergistically inhibits the growth of allogeneic tumors formed from KPC, LLC, or MC-38 cells in mice[1].

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

Animal Model: Subcutaneous injection of 5.0 × 106 MIA PaCa-2 human pancreatic cancer cells into nude mice was performed to establish a tumor xenograft model[1].
Dosage: 75 mg/kg
Administration: I.p., once daily for 35 days
Result: Tumor volume and weight were significantly reduced.
The number of cleaved caspase-3 (apoptosis marker) and 4-HNE (lipid peroxidation marker) positive cells increased, while the number of Cyclin D1 and Ki-67 (proliferation marker) positive cells decreased.
Animal Model: Athymic NCr-nu/nu nude mice were injected orally into the pancreas with 5.0 × 105 luciferase-labeled MIA PaCa-2 cells to form an in situ tumor model that simulates the pancreatic cancer microenvironment[1].
Dosage: 75 mg/kg
Administration: I.p., once daily for 35 days
Result: Tumor growth is inhibited, and tumor weight is reduced.
Animal Model: Athymic NCr-nu/nu nude mice were subcutaneously injected with NCI-H1299 human lung cancer cells or COLO 205 human colon cancer cells to form a xenograft model[1].
Dosage: 75 mg/kg
Administration: I.p., once daily for 35 days
Result: The tumor volume and weight were significantly reduced, and immunohistochemistry showed increased apoptosis and ferroptosis markers.
Animal Model: C57BL/6N mice were subcutaneously injected with KPC (mouse pancreatic cancer cells), LLC (Lewis lung cancer cells), or MC-38 (mouse colon cancer cells) to establish an allogeneic transplantation model[1].
Dosage: 25 mg/kg
Administration: I.p., once daily for 21 days
Result: Combined with aPD-L1, it significantly reduced tumor volume and weight.
PD-L1 expression was increased in tumor tissue, along with increased CD8+ T cell infiltration, elevated IFN-γ and Granzyme B positive cells, while PD-1+ T cells, Treg cells, MDSCs, and TAMs were decreased.
Ki-67 (proliferation) was decreased, and cleaved caspase-3 (apoptosis) was increased.
Molecular Weight

306.68

Formula

C14H8ClFN2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(O)C=C(F)C(C2=CC=C(NC(NC3=O)=O)C3=C2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (326.07 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 3.2607 mL 16.3036 mL 32.6073 mL
5 mM 0.6521 mL 3.2607 mL 6.5215 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (8.15 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 (8.15 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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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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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).
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

Purity: 99.45%

SDS (252 KB)

COA (255 KB) HNMR (142 KB) RP-HPLC (142 KB) LCMS (238 KB)

Handling Instructions (2659 KB)
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. 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 3.2607 mL 16.3036 mL 32.6073 mL 81.5182 mL
5 mM 0.6521 mL 3.2607 mL 6.5215 mL 16.3036 mL
10 mM 0.3261 mL 1.6304 mL 3.2607 mL 8.1518 mL
15 mM 0.2174 mL 1.0869 mL 2.1738 mL 5.4345 mL
20 mM 0.1630 mL 0.8152 mL 1.6304 mL 4.0759 mL
25 mM 0.1304 mL 0.6521 mL 1.3043 mL 3.2607 mL
30 mM 0.1087 mL 0.5435 mL 1.0869 mL 2.7173 mL
40 mM 0.0815 mL 0.4076 mL 0.8152 mL 2.0380 mL
50 mM 0.0652 mL 0.3261 mL 0.6521 mL 1.6304 mL
60 mM 0.0543 mL 0.2717 mL 0.5435 mL 1.3586 mL
80 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0190 mL
100 mM 0.0326 mL 0.1630 mL 0.3261 mL 0.8152 mL
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iMQT_020 Related Classifications

Help & FAQs
  • 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.

Keywords:

iMQT_0202463893-46-9Glutathione PeroxidaseReactive Oxygen Species (ROS)ApoptosisFerroptosisPD-1/PD-L1PD-1/Programmed death-ligand 1SLC1A5_varPD-L1Inhibitorinhibitorinhibit

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