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FDW028

Chemical Structure : FDW028

CAS No.: 2768426-49-7

FDW028 (FDW-028, FDW 028)

Catalog No.: PC-21002Not For Human Use, Lab Use Only.

FDW028 is a potent and highly selective small-molecule inhibitor of fucosyltransferase 8 (FUT8) with binding KD value of 5.486 uM, displays no affinity against other FUTs, shows potent anti-CRC activities.

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Biological Activity

FDW028 is a potent and highly selective small-molecule inhibitor of fucosyltransferase 8 (FUT8) with binding KD value of 5.486 uM, displays no affinity against other FUTs, shows potent anti-CRC activities.
FDW028 exerts potent anti-tumor activities against CRC with IC50 of 5.95 µM and 23.78 µM in SW480 and HCT-8 cells, respectively, significantly represses the migration of SW480 and HCT-8 cells.
FDW028 promotes defucosylation and consequent CMA lysosomal degradation of B7-H3 through CMA pathway.
FDW028 apparently attenuates the expression of both PD-L1 and PD-L2 in CRC cells.
FDW028 attenuates membrane B7-H3 through driving the binding of HSC70 to B7-H3 and consequent autophagolysosomal degradation of B7-H3.
FDW028 (20 mg/kg once the other day, i.v.) prolongs the survival of mice with CRC pulmonary metastases (CRPM).

Physicochemical Properties

M.Wt 388.48
Formula C22H24N6O
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

5-((benzylamino)methyl)-2-((4-ethylbenzyl)amino)-[1,2,4]triazolo[1,5-a]pyrimidin-7-ol

References

1. Wang M, et al. Cell Death Dis. 2023 Aug 3;14(8):495.

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