APTO-253

• UNSPSC Description:

  APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor[1][2]. APTO-253 has antiarthritic activity[3].

• Target Antigen:

  Apoptosis; c-Myc; KLF

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;MAPK/ERK Pathway

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer; Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/APTO-253.html

• Solubility:

  DMSO : 25 mg/mL (ultrasonic;warming;heat to 60°C)

• Smiles:

  CC(N1)=C(C(N2)=NC3=C2C4=CC=CN=C4C5=NC=CC=C53)C6=C1C=CC(F)=C6

• Molecular Weight:

  367.38

• References & Citations:

  [1]Local A, et al. APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells. Mol Cancer Ther. 2018 Jun;17(6):1177-1186.|[2]Hongying Zhang, et al. Inhibition of c-Myc By Apto-253 As an Innovative Therapeutic Approach to Induce Cell Cycle Arrest and Apoptosis in Acute Myeloid Leukemia. Blood 2016 128:1716.|[3]Haruka Tsuchiya, et al. Parsing multiomics landscape of activated synovial fibroblasts highlights drug targets linked to genetic risk of rheumatoid arthritis. Ann Rheum Dis. 2020 Nov2;annrheumdis-2020-218189.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 1

• CAS Number:

  916151-99-0