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Merck
CN

SML4030

FDW028

≥97% (HPLC)

别名:

2-[[(4-Ethylphenyl)methyl]amino]-5-[[(phenylmethyl)amino]methyl][1,2,4]triazolo[1,5-a]pyrimidin-7(1H)-one, 5-[(Benzylamino)methyl]-2-{[(4-ethylphenyl)methyl]amino}[1,2,4]triazolo[1,5-a]pyrimidin-7(4H)-one

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关于此项目

经验公式(希尔记法):
C22H24N6O
化学文摘社编号:
分子量:
388.47
NACRES:
NA.21
Assay:
≥97% (HPLC)
Form:
powder
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Quality Segment

assay

≥97% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

SMILES string

OC1=CC(CNCC2=CC=CC=C2)=NC3=NC(NCC4=CC=C(C=C4)CC)=NN31

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.


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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