Synonym
Nampt-IN-1; Nampt-IN 1; Nampt-IN1; LSN3154567; LSN-3154567; LSN 3154567.
IUPAC/Chemical Name
2-Hydroxy-2-methyl-N-[1,2,3,4-tetrahydro-2-[2-(3-pyridinyloxy)acetyl]-6-isoquinolinyl]-1-propanesulfonamide
InChi Key
QHHSCLARESIWBH-UHFFFAOYSA-N
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
SMILES Code
CC(C)(O)CS(=O)(NC1=CC2=C(CN(C(COC3=CC=CN=C3)=O)CC2)C=C1)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor.
In vitro activity:
This study reports the discovery of a unique NAMPT inhibitor, LSN3154567. This molecule is highly selective and has a potent and broad spectrum of anticancer activity. Its inhibitory activity can be rescued with nicotinic acid (NA) against the cell lines proficient, but not those deficient in NAPRT1, essential for converting NA to NAD+.
Reference: Mol Cancer Ther. 2017 Dec;16(12):2677-2688. https://pubmed.ncbi.nlm.nih.gov/29054982/
In vivo activity:
LSN3154567 also exhibits robust efficacy in multiple tumor mouse models deficient in NAPRT1. Importantly, this molecule when coadministered with NA does not cause observable retinal and hematological toxicities in the rodents, yet still retains robust efficacy.
Reference: Mol Cancer Ther. 2017 Dec;16(12):2677-2688. https://pubmed.ncbi.nlm.nih.gov/29054982/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
250.0 |
595.95 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
419.50
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Zhao G, Green CF, Hui YH, Prieto L, Shepard R, Dong S, Wang T, Tan B, Gong X, Kays L, Johnson RL, Wu W, Bhattachar S, Del Prado M, Gillig JR, Fernandez MC, Roth KD, Buchanan S, Kuo MS, Geeganage S, Burkholder TP. Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration. Mol Cancer Ther. 2017 Dec;16(12):2677-2688. doi: 10.1158/1535-7163.MCT-16-0674. Epub 2017 Oct 20. PMID: 29054982.
In vitro protocol:
1. Zhao G, Green CF, Hui YH, Prieto L, Shepard R, Dong S, Wang T, Tan B, Gong X, Kays L, Johnson RL, Wu W, Bhattachar S, Del Prado M, Gillig JR, Fernandez MC, Roth KD, Buchanan S, Kuo MS, Geeganage S, Burkholder TP. Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration. Mol Cancer Ther. 2017 Dec;16(12):2677-2688. doi: 10.1158/1535-7163.MCT-16-0674. Epub 2017 Oct 20. PMID: 29054982.
In vivo protocol:
1. Zhao G, Green CF, Hui YH, Prieto L, Shepard R, Dong S, Wang T, Tan B, Gong X, Kays L, Johnson RL, Wu W, Bhattachar S, Del Prado M, Gillig JR, Fernandez MC, Roth KD, Buchanan S, Kuo MS, Geeganage S, Burkholder TP. Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration. Mol Cancer Ther. 2017 Dec;16(12):2677-2688. doi: 10.1158/1535-7163.MCT-16-0674. Epub 2017 Oct 20. PMID: 29054982.
1: Zhao G, Green CF, Hui YH, Prieto L, Shepard R, Dong S, Wang T, Tan B, Gong X,
Kays L, Johnson RL, Wu W, Bhattachar S, Del Prado M, Gillig JR, Fernandez MC,
Roth KD, Buchanan S, Kuo MS, Geeganage S, Burkholder TP. Discovery of a Highly
Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal
Toxicity with Nicotinic Acid Co-administration. Mol Cancer Ther. 2017 Oct 20.
pii: molcanther.0674.2016. doi: 10.1158/1535-7163.MCT-16-0674. [Epub ahead of
print] PubMed PMID: 29054982.
