Antitumor agent-83 

Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro^[1].

Antitumor agent-83 (compound 6d) (5-40 µM; 24 h) activates BAX and mediates cell apoptosis, promotes the release cytochrome c in a dose-dependent manner^[1].
Antitumor agent-83 has significant anti-proliferation effect on A549, HCT-116, PC-3, H1581, MDA-MB-231, K562, MV4-11 and THP-1 tumor cells with GI₅₀ values of 2.15 µM, 3.31 µM, 2.50 µM, 2.15 µM, 3.98 µM, 1.41 µM, 2.84 µM, 2.18 µM, respectively^[1].
Antitumor agent-83 (1-5 µM; 24, 48 and 72h) significantly reduces the viability of A549 cells in a dose-and time-dependent manner^[1].
Antitumor agent-83 (5 µM and 10 µM; 48 h) promotes A549 cells apoptosis in a dose-dependent manner^[1].
Antitumor agent-83 (2.5 µM and 5 µM; 48 h) induces cell cycle arrest in G0/G1 phase with dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

494.59

C₂₉H₃₀N₆O₂

CN(C1CCN(CC1)C(C2=CC=C(C=C2)N3N=C(/C(C3=O)=N/NC4=CC=CC=C4)C5=CC=CC=C5)=O)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhang Z, et al. Optimization of BAX trigger site activator BTSA1 with improved antitumor potency and in vitro ADMET properties. Eur J Med Chem. 2023 Feb 15;248:115076.  [Content Brief]