APTO-253

• 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].

• Product Name Alternative :

  LOR-253; LT-253

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  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

• Purity :

  98.86

• 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 Formula :

  C22H14FN5

• Molecular Weight :

  367.38

• Precautions :

  H302, H315, H319, H335

• 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

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• CAS Number :

  [916151-99-0]