MedKoo Cat#: 407339 | Name: LSN3154567
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LSN3154567, also known as Nampt-IN-1, is a potent and elective NAMPT inhibitor. Nicotinamide phosphoribosyltransferase (NAMPT) is a promising antitumor target. NAMPT inhibition leads to attenuation of glycolysis, resulting in further perturbation of carbohydrate metabolism in cancer cells.

Chemical Structure

LSN3154567
LSN3154567
CAS#1698878-14-6

Theoretical Analysis

MedKoo Cat#: 407339

Name: LSN3154567

CAS#: 1698878-14-6

Chemical Formula: C20H25N3O5S

Exact Mass: 419.1515

Molecular Weight: 419.50

Elemental Analysis: C, 57.26; H, 6.01; N, 10.02; O, 19.07; S, 7.64

Price and Availability

Size Price Availability Quantity
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
200mg USD 1,950.00 2 Weeks
500mg USD 3,250.00 2 Weeks
1g USD 4,850.00 2 Weeks
2g USD 6,750.00 2 Weeks
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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
Appearance
Solid powder
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
More Info
Product Data
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
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.

Recalculate based on batch purity %
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.