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NADI-351

Chemical Structure : NADI-351

CAS No.: 2503017-11-4

NADI-351 (NADI 351)

Catalog No.: PC-72454Not For Human Use, Lab Use Only.

NADI-351 is a specific small-molecule inhibitor of Notch1 transcriptional complexes with IC50 of 8.8 uM in cellualr reporter assays.

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Biological Activity

NADI-351 is a specific small-molecule inhibitor of Notch1 transcriptional complexes with IC50 of 8.8 uM in cellualr reporter assays.
NADI-351 inhibited OE33 cell growth in single dose MTT assays (EC50= 10 uM) and, more potently, in multi-dose colony formation assays (EC50=1.3 uM)
NADI-351 is 15 times more potent than IMR-1 in an NTC AlphaScreen assay.
NADI-351 selectively disrupted Notch1 transcription complexes, inhibited recruitment of Notch1 to the NTC (Notch Ternary Complex) and to the HES1 promoter, and reduced Notch1 recruitment to target genes.
NADI-351 inhibits tumor growth in Notch-dependent cancers and does not exert gastrointestinal toxicity associated with goblet cell metaplasia.
NADI-351 selectively inhibits stem-like esophageal adenocarcinoma (EAC) cell populations.

Physicochemical Properties

M.Wt 465.518
Formula C19H20FN5O4S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-2-(5-(1-(4-((4H-1,2,4-triazol-3-yl)methoxy)-3-fluoro-5-methoxyphenyl)ethylidene)-4-oxo-2-thioxothiazolidin-3-yl)-N,N-dimethylacetamide

References

1. Annamil Alvarez-Trotta, et al. Cancer Res. 2021 Jun 15;81(12):3347-3357.

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