Anticancer agent 98 

Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (K_d=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t_1/2>300 min^[1].

Anticancer agent 98 inhibits cancer proliferation among melanoma, breast cancer, and pancreatic cancer with IC50s ranging from 0.6-3 nM^[1].
Anticancer agent 98 (300 nM, 1 μM, or 3 μM; 2 h) increases β-tubulin adduct in PC-3 cells dose-dependently^[1].
Anticancer agent 98 (3.125, 6.25, 12.5, 25, and 50 μM) has high-binding affinity to tubulin proteins with Kd value of 16.9 μM by SPR spectroscopy assay^[1].
Anticancer agent 98 (10 μM, 50 μM; 0-60 min) strongly inhibits tubulin polymerization during 60 min^[1].
Anticancer agent 98 (100 nM; 4 h) has antiproliferative and anti-angiogenesis effect on COS-7 cells in vitro^[1].

In Vitro Metabolic Stability^[1]

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

Anticancer agent 98 (2.5 mg/kg; i.v.; twice per week for 2 weeks) is well tolerated with no significant weight loss in PC3/TxR xenograft tumors in male NSG mice. Anticancer agent 98 also significantly attenuates the progression of prostate cancer tumors, relative to the Paclitaxel (HY-B0015; 10 mg/kg, once weekly) and control groups^[1].

Pharmacokinetic Analysis in NSG Mice^[1]

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

325.37

C₁₇H₁₉N₅O₂

2857070-72-3

O=C1NC2=CC(OC)=CC=C2N(C1)C3=NC(NC)=NC4=C3CCC4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Pochampally S, et al. Design, Synthesis, and Biological Evaluation of Pyrimidine Dihydroquinoxalinone Derivatives as Tubulin Colchicine Site-Binding Agents That Displayed Potent Anticancer Activity Both In Vitro and In Vivo[J]. ACS Pharmacology & Translational Science, 2023.