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APTO-253

CAT: 0804-HY-16291-01Size: 5 mgDry Ice: NoHazardous: No
CAT#: HY-16291-01Size: 5 mg
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PRICE
AVAILABILITY
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1

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