| Description: |
APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death.in vitro: APTO-253 demonstrats potent and selective growth inhibition of a variety of solid tumor cell lines, including colon cancer, non-small cell lung cancer (NSCLC), prostate cancer and melanoma, with IC50 values of 0.04- 2.6 μM. APTO-253 demonstrats even great potency of growth inhibitory activity against leukemia cell lines, including AML, ALL and chronic myeloid leukemia (CML), as well as non-Hodgkin's lymphoma (NHL) cell lines, with IC50 values ranging from 7 nM - 0.3 μM.
in vivo: Nonclinical pharmacology studies have demonstrated that APTO-253 exerts in vivoanti-tumor activity in solid tumors and hematologic cancers. |
