916151-99-0
916151-99-0 structure
- Name: APTO-253
- Chemical Name: lor-253
- CAS Number: 916151-99-0
- Molecular Formula: C22H14FN5
- Molecular Weight: 367.379
- Catalog: Signaling Pathways Cell Cycle/DNA Damage G-quadruplex
- Create Date: 2018-02-01 22:18:53
- Modify Date: 2025-08-20 11:31:41
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APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and also stabilizes Gquadruplex, with anti-proliferative activity.
| Name | lor-253 |
|---|---|
| Synonyms |
2-(5-Fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline
1H-Imidazo[4,5-f][1,10]phenanthroline, 2-(5-fluoro-2-methyl-1H-indol-3-yl)- lor 253 APTO-253 |
| Description | APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and also stabilizes Gquadruplex, with anti-proliferative activity. |
|---|---|
| Related Catalog | |
| Target |
KLF4[1], Gquadruplex[3] |
| In Vitro | APTO-253 is an inducer of KLF4. APTO-253 (5 μM) induces KLF4 expression, and enhances apoptosis induced by cisplatin in both SKOV3 and OVCAR3 cells. APTO-253 (5 μM) also leads to G1 phase arrest and reduces S and G2/M phase cells in SKOV3 and OVCAR3 cells[1]. APTO-253 is cytotoxic to Raji and Raji/253R cell lines, with IC50s of 105 ± 2.4 nM and 1387 ± 94 nM, respectively. APTO-253 (0.5 μM) also causes DNA damage in Raji cells. BRCA1/2 deficient cells are hypersensitive to APTO-253. ABCG2 overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance to APTO-253 in Raji/253R[2]. APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines with IC50s ranging from 57 nM to 1.75 µM. APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down regulates MYC RNA and protein expression in AML lines. APTO-253 (500 nM) leads to DNA damage response pathways in MV4-11 cells. Futhermore, APTO-253 is a potent stabilizer of Gquadruplex (G4) motifs, and demonstrates the greatest propensity for stabilizing the MYC G4 sequences[3]. |
| Cell Assay | Cells are plated and treated with vehicle DMSO or APTO-253 (10 concentrations) in 96 well plates for 5 days at 37°C and 5% CO2. Cell viability is measured using CellTiter 96® AQueous one solution cell proliferation assay, and IC50 values are calculated using GraphPad Prism 7 software[3]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 718.8±70.0 °C at 760 mmHg |
| Molecular Formula | C22H14FN5 |
| Molecular Weight | 367.379 |
| Flash Point | 388.5±35.7 °C |
| Exact Mass | 367.123322 |
| PSA | 70.25000 |
| LogP | 3.33 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.843 |