FDW028
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MedKoo CAT#: 125669

CAS#: 2768426-49-7

Description: FDW028 is a potent and highly selective FUT8 inhibitor. FDW028 evidently prolongs the survival of mice with CRC pulmonary metastases (CRPM). FDW028 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the CMA pathway. Taken together, FUT8 inhibition destabilizes B7-H3 through CMA-mediated lysosomal proteolysis, and FDW028 acts as a potent therapeutic candidate against mCRC by targeting FUT8. FDW028, an inhibitor specifically targeted FUT8, promotes defucosylation and consequent HSC70/LAMP2A-mediated lysosomal degradation of B7-H3, and exhibits potent anti-mCRC activities.

Chemical Structure

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FDW028
CAS# 2768426-49-7
Instruction

Theoretical Analysis

MedKoo Cat#: 125669
Name: FDW028
CAS#: 2768426-49-7
Chemical Formula: C22H24N6O
Exact Mass: 388.20
Molecular Weight: 388.480
Elemental Analysis: C, 68.02; H, 6.23; N, 21.63; O, 4.12

Price and Availability

Size Price Availability Quantity
10mg USD 250 2 Weeks
25mg USD 450 2 Weeks
50mg USD 750 2 Weeks
100mg USD 1250 2 Weeks
200mg USD 2050 2 Weeks
500mg USD 3650 2 Weeks
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Synonym: FDW028; AKOS022054754; HY-155747; CS-0886258; FDW-028; FDW 028

IUPAC/Chemical Name: 5-((benzylamino)methyl)-2-((4-ethylbenzyl)amino)-[1,2,4]triazolo[1,5-a]pyrimidin-7-ol

InChi Key: LJEVZCFIZASGBF-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H24N6O/c1-2-16-8-10-18(11-9-16)14-24-21-26-22-25-19(12-20(29)28(22)27-21)15-23-13-17-6-4-3-5-7-17/h3-12,23,29H,2,13-15H2,1H3,(H,24,27)

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

Appearance: To be determined

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Metastatic colorectal cancer (mCRC) is a major cause of cancer-related mortality due to the absence of effective therapeutics. Thus, it is urgent to discover new drugs for mCRC. Fucosyltransferase 8 (FUT8) is a potential therapeutic target with high level in most malignant cancers including CRC. FUT8 mediates the core fucosylation of CD276 (B7-H3), a key immune checkpoint molecule (ICM), in CRC. FUT8-silence-induced defucosylation at N104 on B7-H3 attracts heat shock protein family A member 8 (HSPA8, also known as HSC70) to bind with 106-110 SLRLQ motif and consequently propels lysosomal proteolysis of B7-H3 through the chaperone-mediated autophagy (CMA) pathway.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 388.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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Wang M, Zhang Z, Chen M, Lv Y, Tian S, Meng F, Zhang Y, Guo X, Chen Y, Yang M, Li J, Qiu T, Xu F, Li Z, Zhang Q, Yang J, Sun J, Zhang H, Zhang H, Li H, Wang W. FDW028, a novel FUT8 inhibitor, impels lysosomal proteolysis of B7-H3 via chaperone-mediated autophagy pathway and exhibits potent efficacy against metastatic colorectal cancer. Cell Death Dis. 2023 Aug 3;14(8):495. doi: 10.1038/s41419-023-06027-0. PMID: 37537172; PMCID: PMC10400579.