SMILES string
OC1=CC(CNCC2=CC=CC=C2)=NC3=NC(NCC4=CC=C(C=C4)CC)=NN31
assay
≥97% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Potent FUT8 inhibitor, demonstrates potent efficacy against metastatic colorectal cancer.
FDW028, a potent and selective FUT8 (fucosyltransferase 8) inhibitor, enhances survival in colorectal cancer metastasis in mice (20 mg/kg, i.v. once the other day) by targeting FUT8 (Kd = 5.486 μM), leading to defucosylation and lysosomal degradation of B7-H3 through the chaperone mediated autophagy pathway in CRC cells. This destabilization is facilitated by increased B7-H3 interactions with HSC70/LAMP2A. FDW-028 shows promising anti-tumor abilities in inhibition of clone formation and cell proliferation in SW480 and HCT-8 cells with IC50 values of 5.95 µM and 23.78 µM, respectively.
FDW028, a potent and selective FUT8 (fucosyltransferase 8) inhibitor, enhances survival in colorectal cancer metastasis in mice (20 mg/kg, i.v. once the other day) by targeting FUT8 (Kd = 5.486 μM), leading to defucosylation and lysosomal degradation of B7-H3 through the chaperone mediated autophagy pathway in CRC cells. This destabilization is facilitated by increased B7-H3 interactions with HSC70/LAMP2A. FDW-028 shows promising anti-tumor abilities in inhibition of clone formation and cell proliferation in SW480 and HCT-8 cells with IC50 values of 5.95 µM and 23.78 µM, respectively.
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