2 Results for "

TOP1-DNA cleavage complexes

" in MedChemExpress (MCE) Product Catalog:
Products (2)

2 Results for "TOP1-DNA cleavage complexes" in MCE Product Catalog:

Cat. No.: HY-188120
AZD5335 is an ADC targeting FRα, with an IC50 of 10.6 nM against human FRα. AZD5335 specifically binds to FRα, mediates internalization and trafficking to lysosomal compartments, while delivering a topoisomerase I inhibitor payload that traps TOP1-DNA cleavage complexes. AZD5335 induces DNA damage response via the ATR, ATM, Chk1 and Chk2 signaling pathways, and increases the levels of phosphorylated KAP1, phosphorylated RPA, phosphorylated γH2AX, as well as PARP cleavage. AZD5335 exhibits bystander cytotoxicity against FRα-negative cells co-cultured with FRα-expressing cells. AZD5335 induces potent and durable responses and complete regression in ovarian cancer models, including models with low FRα expression and models resistant to Elahere, with enhanced efficacy when combined with Carboplatin, Bevacizumab or poly (ADP-ribose) polymerase inhibitors. AZD5335 can be used for ovarian cancer research .
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Cat. No.: HY-184984
CAS No.: 3110372-70-5
Target:  

Topoisomerase

Research Areas:  

Cancer

SN-38-A2 is a topoisomerase I (TOP1) degrader with an IC50 of 6.2 nM in MIA PaCa-2 pancreatic cancer cells. SN-38-A2 mimics protein misfolding via an adamantane hydrophobic tag, hijacks the HSP90 chaperone system, and mediates TOP1 degradation through the ubiquitin-proteasome system. SN-38-A2 assembles with poly β-cyclodextrin to form pH-responsive nanoparticles, enabling site-specific release under the acidic conditions of the tumor microenvironment, and exhibits tumor growth inhibitory effects in MIA PaCa-2 pancreatic cancer and HCT116 colorectal cancer xenograft models. SN-38-A2 can be used in research related to pancreatic cancer, colorectal cancer, and breast cancer .
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