| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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LM10 is a novel, potent and selective inhibitor of tryptophan 2,3-dioxygenase (TDO) with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively. LM10 exhibits selectivity for TDO ver IDO, MAO-A, MAO-B, and a panel of receptors and transporters. LM10 reduces growth of TDO-expressing P815 mastocytoma tumors in mice.
| ln Vivo |
Oral LM10 (160 mg/kg) inhibits the development of P815 tumor cells that express TDO and enhances the rejection of the TDO-negative control clone P815B cl1 [1]. Good competitive inhibition characteristics and TDO inhibition (Ki = 5.6 μM) are demonstrated by LM10 [1]. LM10 exhibits no overt toxicity indicators, is highly soluble and bioavailable, and does not inhibit IDO [1]. After taking 160 mg/kg/day orally, plasma concentrations of LM10 varied between 20 and 40 μg/mL (87-175 μM). This is roughly 40 times greater than the IC50 found in cellular experiments employing physiological tryptophan plasma values [1].
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| Animal Protocol |
Animal/Disease Models: DBA/2 mice (6-8 weeks) [1]
Doses: 160 mg/kg/day Route of Administration: Oral Experimental Results: Prevented the growth of TDO-expressing P815 tumor cells and promoted growth of control clone P815B cl1 Good exclusion, does not express TDO. |
| References |
[1]. Pilotte L, et al. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc Natl Acad Sci U S A. 2012;109(7):2497-2502.
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| Molecular Formula |
C11H8FN5
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|---|---|
| Molecular Weight |
229.2131
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| CAS # |
1316695-35-8
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| SMILES |
FC1=CC2=C(C=C1)C(/C=C/C3=NN=NN3)=CN2
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| InChi Key |
JDBSZVDIUIRSDG-DAFODLJHSA-N
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| InChi Code |
InChI=1S/C11H8FN5/c12-8-2-3-9-7(6-13-10(9)5-8)1-4-11-14-16-17-15-11/h1-6,13H,(H,14,15,16,17)/b4-1+
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| Chemical Name |
6-fluoro-3-[(E)-2-(1H-1,2,3,4-tetrazol-5-yl)ethenyl]-1H-indole
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| Synonyms |
LM10 LM 10 LM-10.
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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) |
DMSO : ~50 mg/mL (~218.14 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 16.67 mg/mL (72.73 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 16 mg/mL (69.80 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3628 mL | 21.8141 mL | 43.6281 mL | |
| 5 mM | 0.8726 mL | 4.3628 mL | 8.7256 mL | |
| 10 mM | 0.4363 mL | 2.1814 mL | 4.3628 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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