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Chemical Structure| 916151-99-0 Chemical Structure| 916151-99-0

Structure of APTO-253
CAS No.: 916151-99-0

Chemical Structure| 916151-99-0

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APTO-253 is a small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Kruppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death.

Synonyms: LT-253; LOR-253

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Product Details of APTO-253

CAS No. :916151-99-0
Formula : C22H14FN5
M.W : 367.38
SMILES Code : CC(N1)=C(C(N2)=NC3=C2C4=CC=CN=C4C5=NC=CC=C53)C6=C1C=CC(F)=C6
Synonyms :
LT-253; LOR-253
MDL No. :MFCD25976826
InChI Key :NIRXBXIPHUTNNI-UHFFFAOYSA-N
Pubchem ID :11960271

Safety of APTO-253

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of APTO-253

cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse aortic vascular smooth muscle cells (MOVAS) 5 µM 24 h APTO-253 reversed the inhibitory effects of quercetin on ox-LDL-induced KLF4-mediated phenotypic switch in MOVAS, increasing lipid accumulation and cholesterol uptake. Int J Mol Sci. 2024 Jul 15;25(14):7755
Corpus cavernosum smooth muscle cells (CCSMCs) 5 µM 48 h APTO-253, as an inducer of KLF4, was introduced for rescue experiments in CCSMCs under the co-culture system World J Mens Health. 2024 Jul;42(3):638-649
Caco-2 cells 1 µM 24 h APTO-253 significantly increased the protein expression of KLF4 in Caco-2 cells, improved TEER and decreased FD4 permeability, and upregulated the protein expression of E-cadherin, Occludin, ZO-1, and Claudin-4 Cell Mol Life Sci. 2024 Nov 29;81(1):470
HCT116 cells 1 µM 24 h Increased γ-H2AFX accumulation in BRCA2-deficient cells Mol Cancer Ther. 2018 Jun;17(6):1167-1176
MCF7 cells 20 µM 24 h Increased γ-H2AFX accumulation in BRCA1-deficient cells Mol Cancer Ther. 2018 Jun;17(6):1167-1176
CAOV3 ovarian carcinoma cells 1 µM 24 h Detected γ-H2AFX foci formation, showing APTO-253 caused DNA damage Mol Cancer Ther. 2018 Jun;17(6):1167-1176
TALL-1 cells 50 nM 72 h APTO-253 induced KLF4 expression and suppressed NOTCH3 expression, promoting differentiation of TALL-1 cells into CD4 single-positive cells followed by apoptotic cell death FASEB J. 2025 May 31;39(10):e70613
MDSCs 50 nM 72 h To evaluate the effect of APTO-253 on KLF4 expression in MDSCs and its regulation of Th17 cell differentiation. Results showed that APTO-253 treatment increased KLF4 expression in MDSCs and reduced Th17 cell numbers. J Diabetes Res. 2021 Sep 15;2021:7945117

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Ob/ob mice Pressure ulcer model Intraperitoneal injection 1 mg/kg Every other day until day 8 To evaluate the effect of APTO-253 on diabetic wound healing. Results showed that APTO-253 significantly accelerated wound healing, increased MDSC populations, and reduced Th17 cell numbers. J Diabetes Res. 2021 Sep 15;2021:7945117

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02267863 Acute Myelogenous Leukemia in ... More >>Relapse|Acute Myelogenous Leukemia, Relapsed, Adult|Acute Myelogenous Leukemia, Adult|Acute Myelogenous Leukemia|High Risk Myelodysplasia Less << PHASE1 TERMINATED 2025-09-21 University of Arizona Cancer C... More >>enter, Tucson, Arizona, 85724, United States|UC San Diego Moores Cancer Center, La Jolla, California, 92093-0698, United States|University of California, Irvine, Orange, California, 92868, United States|Emory University; Winship Cancer Institute, Atlanta, Georgia, 30322, United States|Ochsner Cancer Institute, New Orleans, Louisiana, 70121, United States|University of Michigan, Ann Arbor, Michigan, 48109, United States|St. Vincent Frontier Cancer Center, Billings, Montana, 59102, United States|University of Rochester; Wilmot Cancer Institute Clinical Trials Office, Rochester, New York, 14643, United States|University Hospital, Cleveland, Ohio, 44106, United States|Oregon Health & Science University, Portland, Oregon, 97239, United States|Prisma Health, Institute for Translational Oncology Research, Greenville, South Carolina, 29605, United States|Baylor Research Institute, Dallas, Texas, 75246, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.61mL

2.72mL

1.36mL

27.22mL

5.44mL

2.72mL

References

 

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