Synonym
STF-118804; STF 118804; STF118804.
IUPAC/Chemical Name
4-(5-methyl-4-(tosylmethyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide
InChi Key
DLFCEZOMHBPDGI-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H23N3O4S/c1-17-5-11-22(12-6-17)33(30,31)16-23-18(2)32-25(28-23)21-9-7-20(8-10-21)24(29)27-15-19-4-3-13-26-14-19/h3-14H,15-16H2,1-2H3,(H,27,29)
SMILES Code
O=C(NCC1=CC=CN=C1)C2=CC=C(C3=NC(CS(=O)(C4=CC=C(C)C=C4)=O)=C(C)O3)C=C2
Appearance
White to off-white 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
Biological target:
STF-118804 is a NAMPT inhibitor which reduces the viability of most B-ALL cell lines with IC50 <10 nM.
In vitro activity:
STF-118804 reduced viability and growth of different PDAC (pancreatic ductal adenocarcinoma cell) lines, as well as the formation of colonies in soft agar. In addition, STF-118804 decreased glucose uptake, lactate excretion, and ATP levels, resulting in metabolic collapse. Furthermore, STF-118804 treatment activated AMPK and inhibited of mTOR pathways in these cells.
Reference: Oncotarget. 2017 Jun 29;8(49):85054-85067. https://pubmed.ncbi.nlm.nih.gov/29156703/
In vivo activity:
Panc-1 cells expressing GFP-luciferase were orthotopically implanted on mice pancreas to test the in vivo effectiveness of STF-118804. STF-118804 reduced tumor size after 21 days of treatment. Combinations of STF-118804 with chemotherapeutic agents such as paclitaxel, gemcitabine, and etoposide showed an additive effect in decreasing cell viability and growth. STF-118804 reduced the growth of PDAC in vivo and had an additive effect in combination with main current chemotherapeutic drugs.
Reference: Oncotarget. 2017 Jun 29;8(49):85054-85067. https://pubmed.ncbi.nlm.nih.gov/29156703/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
39.5 |
85.67 |
| DMF |
25.0 |
54.17 |
| DMF:PBS (pH 7.2) (1:5) |
0.2 |
0.43 |
| Ethanol |
1.0 |
2.17 |
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
461.53
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. Espindola-Netto JM, Chini CCS, Tarragó M, Wang E, Dutta S, Pal K, Mukhopadhyay D, Sola-Penna M, Chini EN. Preclinical efficacy of the novel competitive NAMPT inhibitor STF-118804 in pancreatic cancer. Oncotarget. 2017 Jun 29;8(49):85054-85067. doi: 10.18632/oncotarget.18841. PMID: 29156703; PMCID: PMC5689593.
In vitro protocol:
1. Espindola-Netto JM, Chini CCS, Tarragó M, Wang E, Dutta S, Pal K, Mukhopadhyay D, Sola-Penna M, Chini EN. Preclinical efficacy of the novel competitive NAMPT inhibitor STF-118804 in pancreatic cancer. Oncotarget. 2017 Jun 29;8(49):85054-85067. doi: 10.18632/oncotarget.18841. PMID: 29156703; PMCID: PMC5689593.
In vivo protocol:
1. Espindola-Netto JM, Chini CCS, Tarragó M, Wang E, Dutta S, Pal K, Mukhopadhyay D, Sola-Penna M, Chini EN. Preclinical efficacy of the novel competitive NAMPT inhibitor STF-118804 in pancreatic cancer. Oncotarget. 2017 Jun 29;8(49):85054-85067. doi: 10.18632/oncotarget.18841. PMID: 29156703; PMCID: PMC5689593.
1: Vallejo FA, Sanchez A, Cuglievan B, Walters WM, De Angulo G, Vanni S, Graham RM. NAMPT Inhibition Induces Neuroblastoma Cell Death and Blocks Tumor Growth. Front Oncol. 2022 Jun 23;12:883318. doi: 10.3389/fonc.2022.883318. PMID: 35814452; PMCID: PMC9261286.
2: Ogino Y, Sato A, Uchiumi F, Tanuma SI. Cross resistance to diverse anticancer nicotinamide phosphoribosyltransferase inhibitors induced by FK866 treatment. Oncotarget. 2018 Mar 27;9(23):16451-16461. doi: 10.18632/oncotarget.24731. PMID: 29662658; PMCID: PMC5893253.
3: Espindola-Netto JM, Chini CCS, Tarragó M, Wang E, Dutta S, Pal K, Mukhopadhyay D, Sola-Penna M, Chini EN. Preclinical efficacy of the novel competitive NAMPT inhibitor STF-118804 in pancreatic cancer. Oncotarget. 2017 Jun 29;8(49):85054-85067. doi: 10.18632/oncotarget.18841. PMID: 29156703; PMCID: PMC5689593.
4: Deng H, Mi MT. Resveratrol Attenuates Aβ25-35 Caused Neurotoxicity by Inducing Autophagy Through the TyrRS-PARP1-SIRT1 Signaling Pathway. Neurochem Res. 2016 Sep;41(9):2367-79. doi: 10.1007/s11064-016-1950-9. Epub 2016 May 14. PMID: 27180189.
5: Mei SC, Brenner C. NAD as a genotype-specific drug target. Chem Biol. 2013 Nov 21;20(11):1307-8. doi: 10.1016/j.chembiol.2013.11.001. PMID: 24267273; PMCID: PMC3907267.
6: Matheny CJ, Wei MC, Bassik MC, Donnelly AJ, Kampmann M, Iwasaki M, Piloto O, Solow-Cordero DE, Bouley DM, Rau R, Brown P, McManus MT, Weissman JS, Cleary ML. Next-generation NAMPT inhibitors identified by sequential high-throughput phenotypic chemical and functional genomic screens. Chem Biol. 2013 Nov 21;20(11):1352-63. doi: 10.1016/j.chembiol.2013.09.014. Epub 2013 Oct 31. PMID: 24183972; PMCID: PMC3881547.
