LOR 253
LOR 253 Basic information
- Product Name:
- LOR 253
- Synonyms:
-
- LOR 253
- APTO-253
- LOR 253; LOR253; LT-253
- LOR-253; LT-253
- LT-253
- 1H-Imidazo[4,5-f][1,10]phenanthroline, 2-(5-fluoro-2-methyl-1H-indol-3-yl)-
- APTO-253 (LOR-253)
- LT 253,LT253,Myc,c-Myc,inhibit,APTO 253,LOR 253,APTO253,KLF,Apoptosis,Inhibitor,Krüppel-like factor,APTO-253,LOR253
- CAS:
- 916151-99-0
- MF:
- C22H14FN5
- MW:
- 367.38
- Mol File:
- 916151-99-0.mol
LOR 253 Chemical Properties
- Boiling point:
- 718.8±70.0 °C(Predicted)
- Density
- 1.481±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 2 mg/ml; DMSO: 2 mg/ml; Ethanol: insol; PBS (pH 7.2): insol
- form
- A solid
- pka
- 7.75±0.50(Predicted)
- color
- Light yellow to yellow
LOR 253 Usage And Synthesis
Uses
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].
in vivo
APTO-253 (LOR-253; 15 mg/kg; IV; twice per day for 2 consecutive days per week for 14 days) has antiarthritic activity in a CIA model[3].
| Animal Model: | DBA/1J male mice (6 weeks) with collagen induced arthritis (CIA)[3] |
| Dosage: | 15 mg/kg |
| Administration: | IV; twice per day for 2 consecutive days per week for 14 days |
| Result: | Demonstrated significant preventive and therapeutic activity on arthritis formation. |
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. DOI:10.1158/1535-7163.MCT-17-1209
[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. DOI:10.1136/annrheumdis-2020-218189
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