Cas No.: | 916151-99-0 |
Synonyms: | LOR-253; LT-253 |
SMILES: | CC1=C(C2C=C(F)C=CC=2N1)C1=NC2C3C(=NC=CC=3)C3C(=CC=CN=3)C=2N1 |
Formula: | C22H14FN5 |
M.Wt: | 367.38 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |