BOLD-100

BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis , and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.

In Vitro

BOLD-100 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC 50 values of 45-200?μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC 50 value of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC 50 values of 178 μM, 111 μM, and 143 μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL-8, SW480 and HCT116 cells, respectively. BOLD-100 (0-150 μM; 24 hours) induces cell apoptosis alone. When it combines with sorafenib, it increases the numbers of the apopotic cells. Additionally, the p-PARP and caspase 7 cleavage is promoted either. BOLD-100 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Hepatoma, Melanoma, Lung cancer and Colon cancer cell lines Concentration: 0 μM, 50 μM, 100 μM, 150 μM and 200 μM Incubation Time: 72 hours Result: Has anti-cancer activity in diverse malignant tumour cell types. Apoptosis AnalysisCell Line: Hep3B cells Concentration: 0 μM, 75 μM, 150 μM Incubation Time: 72 hours Result: Promoted cell apoptosis as a concentration manner. Western Blot AnalysisCell Line: Hep3B cells Concentration: 0 μM, 75 μM, 150 μM Incubation Time: 72 hours Result: Increased p-STAT3 and p-CREB expression in cells without sorafenib cotreatment.

In Vivo

BOLD-100 (intravenous injection; 30 mg/kg; once a week; 42sdays) combines with the multi-kinase inhibitor sorafenib and exhibits a further anticancer activity when compares to the BOLD-100 treatment alone in Hep3B xenografts grown in Balb/c SCID mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Hep3B xenograft in Balb/c miceDosage: 30 mg/kg Administration: Intravenous injection Result: Had synergistic activity of KP1339 with sorafenib in vivo.

Form:Solid