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TFF3 inhibitor AMPC

Chemical Structure : TFF3 inhibitor AMPC

CAS No.: 2254434-33-6

TFF3 inhibitor AMPC (AMPC)

Catalog No.: PC-38711Not For Human Use, Lab Use Only.

AMPC is a first-in-class small-molecule inhibitor of the oncogenic functions of trefoil factor 3 (TFF3) that specifically monomerizes dimeric TFF3 to inhibit dimeric TFF3 function, specifically binds to Cys57 of TFF3.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AMPC is a first-in-class small-molecule inhibitor of the oncogenic functions of trefoil factor 3 (TFF3) that specifically monomerizes dimeric TFF3 to inhibit dimeric TFF3 function, specifically binds to Cys57 of TFF3.
AMPC treatment decreased TFF3 protein levels in a dose-dependent manner in BT474 cells, with a significant reduction of TFF3 levels at 10 uM, decreased HER1-4 phosphorylation and phosphorylation of downstream AKT and p44/42 MAPK in a dose-dependent manner.
AMPC exhibited cell growth inhibition against BT474 and MDA-MB-361 cells with IC50 of 1.2 and 3.7 uM, respectively.
AMPC inhibition of TFF3 decreased monolayer cell viability, increased apoptosis and decreased 3D Matrigel growth of trastuzumab resistant BT474 cells, without re-sensitization to trastuzumab.
AMPC exhibited synergistic inhibitory effects on lung ADC cell growth when combined with various MEK1/2 inhibitors.

Physicochemical Properties

M.Wt 425.419
Formula C25H16FN3O3
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

2-Amino-4-(4-(6-fluoro-5-methylpyridin-3-yl)phenyl)-5-oxo-4H,5H-pyrano[3,2-c]chromene-3-carbonitrile

References

1. Chong QY, et al. Oncotarget. 2017;8:74188–74208.

2. Mengyi Zhang, et al. Oncogenesis. 2019 Nov 4;8(11):65.

3. Poh HM, et al. Cancers (Basel). 2019 Oct 10;11(10):1528.

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