| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
iMQT_020 showed the strongest inhibitory effect on mitochondrial glutamine uptake at a concentration of 10 μM (IC50 = 6.156 μM)[1]. iMQT_020 (0-100 μM) can bind directly to wild-type SLC1A5_var protein (Kd = 4.473 μM), but not to FIL/AAA mutant[1]. iMQT_020 (4 μM) can significantly reduce the circular dichroism (CD) signal of wild-type SLC1A5_var protein, indicating that its structure has been altered[1]. iMQT_020 (10 μM) can reduce the levels of glutamine-derived tricarboxylic acid cycle metabolites (such as glutamate, α-ketoglutarate, succinic acid, etc.) and their downstream products (such as glutathione, proline) in MIA PaCa-2 cells[1]. iMQT_020 (10 μM, 24 hours) reduced GSH levels in MIA PaCa-2 cells and increased intracellular and mitochondrial ROS levels [1]. iMQT_020 (10 μM, 24 hours) reduced oxygen consumption rate (OCR) and extracellular acidification rate (ECAR) in MIA PaCa-2 cells overexpressing SLC1A5_var WT, but had no effect on FIL/AAA mutants [1]. iMQT_020 (10 μM, 24 hours) altered mitochondrial morphology in MIA PaCa-2 cells (reduced mitochondrial fragmentation) and reduced mitochondrial membrane potential (reduced TMRE staining) [1]. iMQT_020 (48 hours) selectively inhibited cancer cell viability (IC50 5-40 μM) without affecting normal cells [1]. iMQT_020 (10 μM, 24 h) can upregulate the expression of PD-L1 mRNA and protein in human PDAC cell lines (such as SU.86.86, SW1990) and mouse cancer cell lines (KPC, LLC, MC-38) [1].
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| ln Vivo |
iMQT_020 (75 mg/kg, intraperitoneal injection, once daily for 35 days) inhibited tumor growth in the MIA PaCa-2 cell xenograft model by inducing cell hiding and ferroptosis [1]. iMQT_020 (75 mg/kg, intraperitoneal injection, once daily for 35 days) inhibited tumor growth in the MIA PaCa-2 cell xenograft model by inducing cell retention and ferroptosis [1]. iMQT_020 (75 mg/kg, intraperitoneal injection, once daily for 35 days) inhibited tumor growth in NCI-H1299 human lung cancer cells and COLO 205 human cardiovascular xenograft tumors [1]. iMQT_020 (25 mg/kg, intraperitoneal injection, once daily for 21 days) effectively inhibited the growth of allogeneic tumors of KPC, LLC or MC-38 cells in mice when used in combination with anti-PD-L1 reagent (aPD-L1) [1].
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| Animal Protocol |
Animal/Disease Models: 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].
Doses: 75 mg/kg Route of Administration: I.p., once daily for 35 days Experimental Results: 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/Disease Models: 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]. Doses: 75 mg/kg Route of Administration: I.p., once daily for 35 days Experimental Results: Tumor growth is inhibited, and tumor weight is reduced. Animal/Disease Models: 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]. Doses: 75 mg/kg Route of Administration: I.p., once daily for 35 days Experimental Results: The tumor volume and weight were significantly reduced, and immunohistochemistry showed increased apoptosis and ferroptosis markers. Animal/Disease Models: 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]. Doses: 25 mg/kg Route of Administration: I.p., once daily for 21 days Experimental Results: 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. |
| References |
| Molecular Formula |
C14H8CLFN2O3
|
|---|---|
| Molecular Weight |
306.68
|
| CAS # |
2463893-46-9
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| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3261 mL | 1.6304 mL | 3.2607 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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