916151-99-0
Chemical Structure
APTO-253
Synonym(s): LOR-253; LT-253
- CAS No.: 916151-99-0
- Formula:C22H14FN5
- Molecular Weight:367.38
IUPAC Name: 2-(5-fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline
InChIKey: NIRXBXIPHUTNNI-UHFFFAOYSA-N
SMILES: CC(N1)=C(C(N2)=NC3=C2C4=CC=CN=C4C5=NC=CC=C53)C6=C1C=CC(F)=C6
Biological Activity: 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].
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APTO-253 | 99.74% | 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. APTO-253 has antiarthritic activity. | ||||||||||||||||||||
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Similarity Score 1.00
HY-16291AAPTO-253 hydrochloride -
Similarity Score 0.64
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HY-W1130302-(Pyridin-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline -
Similarity Score 0.63
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HY-W1124964-(1H-Imidazo[4,5-f][1,10]phenanthrolin-2-yl)benzoic acid -
Similarity Score 0.63
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HY-W1127012-(1H-Imidazo[4,5-f][1,10]phenanthrolin-2-yl)benzoic acid -
Similarity Score 0.60
HY-181560SLD1121 -
Similarity Score 0.55
HY-16332ML-220 -
Similarity Score 0.53
HY-W0754505,5'-Bi(1,10-phenanthroline) -
Similarity Score 0.52
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HY-W034636Dipyrido[3,2-a:2',3'-c]phenazine -
Similarity Score 0.52
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HY-W456457Tetrapyrido[3,2-a:2',3'-c:3'',2''-h:2''',3'''-j]phenazine -
Explore the MedChemAI to find more analogs
![2-(Pyridin-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline Chemical Structure](http://file.medchemexpress.com/product_pic/hy-w113030.gif)
![4-(1H-Imidazo[4,5-f][1,10]phenanthrolin-2-yl)benzoic acid Chemical Structure](http://file.medchemexpress.com/product_pic/hy-w112496.gif)
![2-(1H-Imidazo[4,5-f][1,10]phenanthrolin-2-yl)benzoic acid Chemical Structure](http://file.medchemexpress.com/product_pic/hy-w112701.gif)
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References
- [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]. 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. [Content Brief]
