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COA of N-65828

Description:

NCI-65828 (designated as N 65828,NSC-65828) is a small-molecule inhibitor targeting angiogenin (ANG), a protein critical for angiogenesis and cellular proliferation. Its therapeutic potential stems from selective suppression of ANG's ribonucleolytic function, a biochemical activity essential for mediating downstream biological effects. By disrupting ANG's enzymatic capacity to cleave RNA substrates, NCI-65828 attenuates the protein's pro-angiogenic signaling pathways. Preclinical evaluations highlight its multifaceted antitumor properties. In vitro studies using diverse cancer cell models—including bladder carcinoma (T24; IC₅₀ = 1.3 ± 0.5 μM), cervical adenocarcinoma (HeLa; IC₅₀ = 1.9 ± 0.4 μM), and urothelial carcinoma (UROtsa; IC₅₀ = 3.2 ± 0.8 μM)—demonstrate dose-dependent antiproliferative effects, with potency variations reflecting tissue-specific sensitivity. Parallel experiments in human umbilical vein endothelial cells (HUVECs) reveal significant inhibition of capillary-like tube formation, confirming its antiangiogenic efficacy in disrupting endothelial morphogenesis. Notably, in vivo investigations using transgenic murine models demonstrate that NCI-65828 effectively suppresses the development of prostatic intraepithelial neoplasia (PIN) lesions. Mechanistic analysis indicates this activity arises from direct enzymatic inhibition rather than interference with ANG's intracellular trafficking, as nuclear translocation remains unaffected—a distinguishing feature that differentiates it from other ANG-targeted agents. This selective mode of action positions NCI-65828 as a precision tool for studying ANG-dependent pathologies.

Chemical Information

Catalog Featured products
Purity of current batch >98%
CAS 501444-06-0
Molecular Weight (MW) 419.453083753586
Molecular Formula C22H17N3O4S
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Handling:

Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

Reference:

A small-molecule inhibitor of the ribonucleolytic activity of human angiogenin that possesses antitumor activity-PNAS-July 23, 2002 vol. 99 no. 15