UNBS5162

UNBS5162的生物活性

UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
IC50 value: 4.7-46.5 uMcancer cell line) [1]
Target: CXCL regulator
in vitro: The mean antiproliferative activity IC50 values determined against nine human cancer cell lines investigated (using the MTT colorimetric assay) were 19.8 and 17.9 μM for UNBS3157 and UNBS5162, respectively [1].
in vivo: In the PC-3 model, UNBS3157 displayed appreciable activity against PC-3 prostate carcinoma when administered orally at 160 mg/kg (%T/C: 151%, P = .03) but not at the lower dose of 40 mg/kg (%T/C: 100%). Repeat i.v. administration of the compound at 10 mg/kg (three times a week for 6 consecutive weeks) contributed therapeutic benefits that were similar to repeat i.v. administration (once a week for 6 consecutive weeks) of 20-mg/kg taxol in the PC-3 orthotopic model [1]. UNBS5162 was administered in a 3 + 3 dose escalation scheme by intravenous infusion over 1 h weekly for 3 weeks of a 4-week cycle. Safety, serial serum PK and tolerability were captured throughout the study. Response Evaluation Criteria in Solid Tumors was utilized every 2 cycles to assess for anti-tumor response [2].