LM10
Based on 1 publication(s) in Google Scholar
LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO). Tryptophan 2,3-dioxygenase (TDO) is an unrelated hepatic enzyme that also degrades tryptophan along the kynurenine pathway. LM10 has the potential for the research of cancer diseases.
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- Pureza: 99.94%
- No. CAS: 1316695-35-8
- Fòrmula: C11H8FN5
- Peso molecular:229.22
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) LM10
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Actividad biológica
TDO[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.398 μM
Compound: LM10
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Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
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[PMID: 30321802] |
| P815 | IC50 |
>100 μM
Compound: LM10
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Inhibition of mouse IDO1 in P815 clone 6 cells by HPLC analysis
Inhibition of mouse IDO1 in P815 clone 6 cells by HPLC analysis
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[PMID: 22616902] |
| P815 | IC50 |
17 μM
Compound: LM10
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Inhibition of mouse TDO in P815 clone 12 cells by HPLC analysis
Inhibition of mouse TDO in P815 clone 12 cells by HPLC analysis
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[PMID: 22616902] |
| U-87MG ATCC | IC50 |
0.671 μM
Compound: LM10
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Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
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[PMID: 30321802] |
LM10 displays a good TDO inhibition (Ki = 5.6 μM) with a competitive inhibition profile[1].
LM10 does not inhibit IDO and has a high solubility and bioavailability without obvious signs of toxicity[1].
The plasma concentration of LM10 after oral administration of 160 mg/kg/day is between 20 and 40 μg/mL (87-175 μM), a concentration about 40 times above the IC50 measured in the cellular assay performed with the physiological concentration of plasma tryptophan[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2 mice (6-8 weeks)[1]
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Dosage:160 mg/kg/day
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Administration:p.o.
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Result:Prevented the growth of TDO-expressing P815 tumor cells and promoted better rejection of control clone P815B cl1, which does not express TDO.
Chemical Information
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No. CAS 1316695-35-8
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Appearance Solid
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Peso molecular 229.22
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Fòrmula C11H8FN5
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Color Off-white to yellow
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SMILES
FC1=CC2=C(C=C1)C(/C=C/C3=NN=NN3)=CN2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
Peritumoural adipose tissue promotes ferroptosis resistance by 3-hydroxykynurenine-mediated suppression of ferritinophagy. [Abstract]2026 Apr;28(4):783-796. PMID: 41813885
Solvente y solubilidad
DMSO : 50 mg/mL (218.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (10.91 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 (10.91 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (622 KB)
- English - EN (622 KB)
- Français - FR (622 KB)
- Deutsch - DE (622 KB)
- Norwegian - NO (622 KB)
- Español - ES (622 KB)
- Swedish - SV (622 KB)
- Italian - IT (622 KB)
- Korean - KR (622 KB)
- Portuguese - PT (622 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 4.3626 mL | 21.8131 mL | 43.6262 mL | 109.0655 mL |
| 5 mM | 0.8725 mL | 4.3626 mL | 8.7252 mL | 21.8131 mL | |
| 10 mM | 0.4363 mL | 2.1813 mL | 4.3626 mL | 10.9066 mL | |
| 15 mM | 0.2908 mL | 1.4542 mL | 2.9084 mL | 7.2710 mL | |
| 20 mM | 0.2181 mL | 1.0907 mL | 2.1813 mL | 5.4533 mL | |
| 25 mM | 0.1745 mL | 0.8725 mL | 1.7450 mL | 4.3626 mL | |
| 30 mM | 0.1454 mL | 0.7271 mL | 1.4542 mL | 3.6355 mL | |
| 40 mM | 0.1091 mL | 0.5453 mL | 1.0907 mL | 2.7266 mL | |
| 50 mM | 0.0873 mL | 0.4363 mL | 0.8725 mL | 2.1813 mL | |
| 60 mM | 0.0727 mL | 0.3636 mL | 0.7271 mL | 1.8178 mL | |
| 80 mM | 0.0545 mL | 0.2727 mL | 0.5453 mL | 1.3633 mL | |
| 100 mM | 0.0436 mL | 0.2181 mL | 0.4363 mL | 1.0907 mL |
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