Formulation: A solid
Formal Name: 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl-2H-1-benzopyran-6-carboxamide
Purity: ≥98%
Formula Markup: C27H34N2O5
Formula Weight: 466,6
Shelf life (days): 1460
CAS Number: 2411429-33-7
Notes: NCT-58 is an inhibitor of heat shock protein 90 (Hsp90).{65713,65714} It binds to the C-terminal domain of Hsp90α and inhibits the protein-protein interaction between the Hsp90α C-terminal domain and peptidylprolyl isomerase D (PPID), a co-chaperone. It decreases cell viability and induces apoptosis in HER2-positive BT474 and SK-BR-3 human breast cancer cells when used at concentrations ranging from 0.5 to 20 µM.{65713} NCT-58 (10 µM) reduces mammosphere formation by, as well as heat shock factor 1 (Hsf1), Hsp70, and Hsp90 protein levels in, BT474 cells. It also reduces intratumoral levels of HER2 and the intracellular domain of HER2 (ICD-HER2), as well as reduces tumor growth and angiogenesis, in a trastuzumab-resistant JIMT-1 breast cancer mouse xenograft model when administered at a concentration of 30 mg/kg.
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