Antiproliferative agent-23 

Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity^[1].

Antiproliferative agent-23 (72 hours) has vitro antiproliferative effect in HepG2 (IC₅₀=0.86), MDA-MB-231 (IC₅₀=1.53), MCF-7 (IC₅₀=0.94), A2780 (IC₅₀=0.88), A549 (IC₅₀=0.23), A549/CDDP (IC₅₀=0.35), HepG2/CDDP (IC₅₀=1.16), HUEVC (IC₅₀=5.68)^[1].
Antiproliferative agent-23 (5 μM; 24 hours) effectively induces cell apoptosis in A549/CDDP cells^[1].
Antiproliferative agent-23 (5 μM; 24 hours) can efficiently cause DNA damage in A549/CDDP cells and thus ultimately triggered apoptosis. Antiproliferative agent-23 causes a significant increase in the ER stress-related protein expression^[1].
Antiproliferative agent-23 (10, 20 μM; 24 hours) leads to inhibitory effects of polymerization with an IC₅₀ of 9.86 μM^[1].
Antiproliferative agent-23 (5 μM; 24 hours) significantly increases intracellular ROS in A549/CDDP cells^[1].
Antiproliferative agent-23 (1 μM; 24 hours) potently inhibits A549 cell migration in in vitro assays^[1].

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

Antiproliferative agent-23 (12.40 mg/kg; IV; every 7 days for 28 consecutive days) has antitumor efficacy and retaines the high antitumor efficiency to attenuate CDDP resistance^[1].

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

743.93

C₂₃H₂₈Cl₃N₃O₆Pt

3049213-47-7

O=C(C1=CC(OC)=C(C(OC)=C1)OC)/C=C/C2=CC=CC3=C2C=CN3CCC(O[Pt](Cl)(Cl)(Cl)([NH3])[NH3])=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhikun Liu, et al. Novel Indole-Chalcone Derivative-Ligated Platinum(IV) Prodrugs Attenuate Cisplatin Resistance in Lung Cancer through ROS/ER Stress and Mitochondrial Dysfunction. J Med Chem. 2023 Apr 13;66(7):4868-4887.  [Content Brief]