APTO-253

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 Specifications

CAS Number

[916151-99-0]

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.