Synonym
FDW028; 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.
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.
| 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 |
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.
