iMQT_020
Based on 1 Customer Validation
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.
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- Purity: 99.45%
- CAS No.: 2463893-46-9
- 화학식: C14H8ClFN2O3
- 분자량:306.68
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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NF-κB Signaling Compound Library
HY-L014
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Anti-Cancer Compound Library
HY-L025
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Small Molecule Immuno-Oncology Compound Library
HY-L031
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Anti-Aging Compound Library
HY-L034
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Antioxidant Compound Library
HY-L037
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Oxygen Sensing Compound Library
HY-L045
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Ferroptosis Compound Library
HY-L051
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Cancer Metabolism Compound Library
HY-L083
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Anti-Colorectal Cancer Compound Library
HY-L103
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Cuproptosis Compound Library
HY-L133
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Metabolic Enzyme Compound Library
HY-L146
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Ovarian Cancer Compound Library
HY-L173
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Multi-Target Compound Library
HY-L176
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Radioprotector Library
HY-L178
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
Biological Activity
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 (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.
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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].
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Dosage:75 mg/kg
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Administration:I.p., once daily for 35 days
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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.
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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].
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Dosage:75 mg/kg
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Administration:I.p., once daily for 35 days
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Result:Tumor growth is inhibited, and tumor weight is reduced.
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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].
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Dosage:75 mg/kg
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Administration:I.p., once daily for 35 days
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Result:The tumor volume and weight were significantly reduced, and immunohistochemistry showed increased apoptosis and ferroptosis markers.
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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].
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Dosage:25 mg/kg
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Administration:I.p., once daily for 21 days
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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.
Chemical Information
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CAS No. 2463893-46-9
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Appearance Solid
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분자량 306.68
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화학식 C14H8ClFN2O3
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Color White to off-white
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SMILES
ClC1=C(O)C=C(F)C(C2=CC=C(NC(NC3=O)=O)C3=C2)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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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