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  3. FDW028

FDW028 a potent and highly selective FUT8 inhibitor. FUT8 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. FDW028 can be used for metastatic colorectal cancer (mCRC) research.

For research use only. We do not sell to patients.

FDW028 Chemical Structure

FDW028 Chemical Structure

CAS No. : 2768426-49-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

FDW028 a potent and highly selective FUT8 inhibitor. FUT8 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. FDW028 can be used for metastatic colorectal cancer (mCRC) research[1].

In Vitro

FDW028 (50 μM, 72 hours) promotes defucosylation and lysosomal degradation of B7-H3 and inhibits the AKT/MTOR pathway[1].
FDW028 (50 μM, 72 hours) promotes B7-H3 and LAMP1 colocalization, facilitating lysosomal degradation of B7-H3[1].
FDW028 (0.2–100 μM, 72 hours) significantly inhibits proliferation of SW480 and HCT-8 cells with IC50 values of 5.95 μM and 23.78 μM[1].
FDW028 (50 μM, 72 hours) significantly inhibits migration in SW480 and HCT-8 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence[1]

Cell Line: SW480 cells, HCT-8 cells
Concentration: 0.2–100 μM
Incubation Time: 72 h
Result: Promoted the colocalization of B7-H3 and LAMP1 in lysosomes.

Cell Proliferation Assay[1]

Cell Line: SW480 cells, HCT-8 cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Inhibited cell proliferation, with IC50 values of 5.95 μM and 23.78 μM for SW480 and HCT-8, respectively.

Western Blot Analysis[1]

Cell Line: SW480 cells, HCT-8 cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Promoted defucosylation of B7-H3, facilitated lysosomal degradation, and inhibited the AKT/MTOR pathway.

Cell Migration Assay [1]

Cell Line: SW480 cells, HCT-8 cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Inhibited the migration ability of SW480 and HCT-8 cells.
In Vivo

FDW028 (10 or 20 mg/kg, i.v. every other day) exhibits significant anti-tumor activity in the SW480 xenograft mouse model[1].
FDW028 (20 mg/kg, i.v. every other day) significantly prolongs survival in the Mc38 pulmonary metastasis model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Colorectal cancer cell line SW480 xenograft mouse model (C57BL/6 mice, 4-6 weeks)[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Intravenous injection (i.v.), every other day, tumor size and body weight were measured every other day during the experiment
Result: Inhibited tumor growth, comparable to 5-Fu (HY-90006), and did not cause significant weight loss.
Animal Model: Mc38 colorectal cancer pulmonary metastasis mouse model (C57BL/6 mice, 4-6 weeks)[1]
Dosage: 20 mg/kg
Administration: Intravenous injection (i.v.), every other day, were measured every other day during the experiment
Result: Significantly prolonged the survival of tumor-bearing mice.
Molecular Weight

388.47

Formula

C22H24N6O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (257.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5742 mL 12.8710 mL 25.7420 mL
5 mM 0.5148 mL 2.5742 mL 5.1484 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.51%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5742 mL 12.8710 mL 25.7420 mL 64.3550 mL
5 mM 0.5148 mL 2.5742 mL 5.1484 mL 12.8710 mL
10 mM 0.2574 mL 1.2871 mL 2.5742 mL 6.4355 mL
15 mM 0.1716 mL 0.8581 mL 1.7161 mL 4.2903 mL
20 mM 0.1287 mL 0.6436 mL 1.2871 mL 3.2178 mL
25 mM 0.1030 mL 0.5148 mL 1.0297 mL 2.5742 mL
30 mM 0.0858 mL 0.4290 mL 0.8581 mL 2.1452 mL
40 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6089 mL
50 mM 0.0515 mL 0.2574 mL 0.5148 mL 1.2871 mL
60 mM 0.0429 mL 0.2145 mL 0.4290 mL 1.0726 mL
80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8044 mL
100 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6436 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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FDW028
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