STF-118804
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MedKoo CAT#: 406581

CAS#: 894187-61-2

Description: STF-118804 is a potent and highly specific NAMPT inhibitor ( nicotinamide phosphoribosyl transferase inhibitor), which improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and targets leukemia stem cells.


Chemical Structure

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STF-118804
CAS# 894187-61-2

Theoretical Analysis

MedKoo Cat#: 406581
Name: STF-118804
CAS#: 894187-61-2
Chemical Formula: C25H23N3O4S
Exact Mass: 461.14093
Molecular Weight: 461.53
Elemental Analysis: C, 65.06; H, 5.02; N, 9.10; O, 13.87; S, 6.95

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 650.0 Ready to ship
200.0mg USD 950.0 Ready to ship
500.0mg USD 1650.0 Ready to ship
1.0g USD 2850.0 Ready to ship
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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://www.ncbi.nlm.nih.gov/pmc/articles/PMC5689593/
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. Overall these results show that the NAMPT inhibitor STF-118804 reduced the growth of PDAC in vitro and in vivo and had an additive effect in combination with main current chemotherapeutic drugs. Reference: Oncotarget. 2017 Jun 29;8(49):85054-85067. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5689593/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.54 85.67
DMF 25.0 54.17
DMF:PBS (pH 7.2) (1:5) 0.2 0.43
Ethanol 1.0 2.17

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.

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. 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.

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1: 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. PubMed PMID: 24267273; PubMed Central PMCID: PMC3907267.



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