APTO-253
Product Specifications
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
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-16291/APTO-253-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-16291/APTO-253-SDS-MedChemExpress.pdf
Clinical Information
Phase 1
CAS Number
916151-99-0
Available Sizes
Curated Selection
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