APTO-253 (hydrochloride)
APTO-253 (LOR-253) hydrochloride 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 hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4 (KLF4) tumor suppressor. APTO-253 hydrochloride exhibits antiarthritic activity[1].
Product Specifications
CAS Number
1691221-67-6
Product Name Alternative
LOR-253 (hydrochloride) ; LT-253 (hydrochloride)
UNSPSC
12352005
Target
C-Myc
Type
Reference compound
Related Pathways
Apoptosis
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/apto-253-hydrochloride.html
Smiles
CC(NC1=C2C=C(F)C=C1)=C2C3=NC4=C5C=CC=NC5=C6N=CC=CC6=C4N3
Molecular Formula
C22H14FN5
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. [Content Brief]|[2]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.|[3]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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 1
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