NSC 850745 is a selective and potent inhibitor of c-Met/STAT3, with IC50 values of 210 nM and 670 nM, respectively. It inhibits cell proliferation, induces G2/M phase arrest, and triggers apoptosis (cell death). NSC 850745 downregulates the expression of AKT-1, VEGF, and Bcl-2, while modulating p53, Bax, and caspase levels. This compound is utilized in cancer research, including studies on leukemia and colon cancer.

NSC 850745 (Compound 22b) exhibits sub-group mean values of GI 50, TGI, and LC 50 at 6.97, 17.15, and 43.56 μM against leukemia cells. It demonstrates the highest potency against EKVX (non-small cell lung cancer) and CAKI-1 (renal cancer cells), with GI 50 values of 1.1 and 1.17 μM, respectively. At a concentration of 10 μM, NSC 850745 inhibits the phosphorylation of c-Met and STAT3 by 96.9% and 95.7%. For HCT-116 colon cancer cells, it has an IC 50 of 2.41 μM, while showing an IC 50 of 56.25 μM for normal WI-38 fibroblast cells, resulting in a selectivity index of 23.3. Administered at 2.41 μM for 24 hours, NSC 850745 induces G2/M phase arrest and triggers late apoptosis and necrosis in HCT-116 cells. Additionally, at the same concentration and duration, it downregulates AKT-1, VEGF, and Bcl-2 gene expression while upregulating the expression of p53, PUMA, Bax, Cyto-C, caspase-3, caspase-8, and caspase-9. NSC 850745 also decreases ATPase activity in HCT-116 cells at 2.41 μM over 24 hours.