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LSN3154567 (LSN-3154567; Nampt-IN-1) is a novel and potent Nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with potential anticancer activity. It inhibits NAMPT with IC50 of 18 nM (NCI-H1155 cell), 49 nM (Calu-6 cell), 333 nM (HCC1937 cell), and 389 nM (MCF-7 cell), respectively.
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| ln Vitro |
LSN3154567 was evaluated in a range of biochemical and cellular assays to assess its selectivity, specificity, and impact on cellular NAD+ levels. Purified NAMPT is inhibited by LSN3154567 at an IC50 of 3.1 nM. It eliminated CSF1R (IC50≈0.84 μM) when evaluated against a panel of human kinases (>100; CEREP Kinase Panel). Broad-spectrum anticancer action is exhibited by LSN3154567. LSN3154567 was tested against a variety of cancer cell lines that were either cultivated with or without nicotinic acid (NA) (10 μM) in order to assess its anticancer potential. LSN3154567 has strong antiproliferative action against a variety of cell lines when NA is not present [1].
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| ln Vivo |
Nampt-IN-1 (LSN3154567) is an oral medication with good physicochemical characteristics. Its plasma exposure was 195 nM*h with a peak concentration of 57 nM (at 0.25 h) and an oral bioavailability of 39% when given orally to mice at a dose of 2 mg/kg. The liver clearance was 158.73 mL/min/kg and the volume of distribution was 7.1 L/kg when the intravenous dose of 2 mg/kg was given. It is calculated that the terminal elimination half-life is 2.76 hours. LSN3154567 has an estimated TED50 value of 2.0 mg/kg and inhibits NAD+ production in a dose-dependent manner. Rats were given LSN3154567 at doses of 20, 40, and 80 mg/kg for four days in order to determine whether the drug induces retinopathy. There was no discernible retinopathy found. Be mindful of hematological toxicity. Plasma doses of 8,974, 18,061 and 38,327 M*h were measured at 20, 40 and 80 mg/kg of LSN3154567, respectively. As a result, LSN3154567's exposure folds were 3, 7, and 14 times, respectively, greater than the exposure (2,701 M*h) needed to attain high efficacy (≈103%) without simultaneous NA delivery. Dogs received LSN3154567 at doses of 1 and 2.5 mg/kg. It was shown that these dosage levels caused retinal toxicity. All four animals had outer nuclear layer degeneration, albeit it was less severe in those given 1 mg/kg. At dose levels of 1 and 2.5 mg/kg, the plasma exposure was found to be 1,483 and 2,468 nM*h, respectively [1].
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| Cell Assay |
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| References |
| Molecular Formula |
C20H25N3O5S
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| Molecular Weight |
419.496
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| Exact Mass |
419.151
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| CAS # |
1698878-14-6
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| PubChem CID |
92044379
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
659.9±65.0 °C at 760 mmHg
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| Flash Point |
352.9±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.624
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| LogP |
0.97
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
664
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QHHSCLARESIWBH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25N3O5S/c1-20(2,25)14-29(26,27)22-17-6-5-16-12-23(9-7-15(16)10-17)19(24)13-28-18-4-3-8-21-11-18/h3-6,8,10-11,22,25H,7,9,12-14H2,1-2H3
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| Chemical Name |
2-hydroxy-2-methyl-N-[2-(2-pyridin-3-yloxyacetyl)-3,4-dihydro-1H-isoquinolin-6-yl]propane-1-sulfonamide
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| Synonyms |
Nampt-IN1 Nampt-IN 1 Nampt-IN-1LSN3154567 LSN-3154567
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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) |
DMSO : ~250 mg/mL (~595.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.96 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 20.8 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: ≥ 2.08 mg/mL (4.96 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 20.8 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: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3838 mL | 11.9190 mL | 23.8379 mL | |
| 5 mM | 0.4768 mL | 2.3838 mL | 4.7676 mL | |
| 10 mM | 0.2384 mL | 1.1919 mL | 2.3838 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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