LOR 253
- Product Name
- LOR 253
- CAS No.
- 916151-99-0
- Chemical Name
- LOR 253
- Synonyms
- LT-253;LOR 253;APTO-253;LOR-253; LT-253;APTO-253 (LOR-253);LOR 253; LOR253; LT-253;APTO-253, 10 mM in DMSO;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)-;LT 253,LT253,Myc,c-Myc,inhibit,APTO 253,LOR 253,APTO253,KLF,Apoptosis,Inhibitor,Krüppel-like factor,APTO-253,LOR253
- CBNumber
- CB82628042
- Molecular Formula
- C22H14FN5
- Formula Weight
- 367.38
- MOL File
- 916151-99-0.mol
LOR 253 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- BA166663
- Product name
- APTO 253
- Packaging
- 10mg
- Price
- $135
- Updated
- 2021/12/16
- Product number
- CS-5226
- Product name
- APTO-253
- Purity
- 98.15%
- Packaging
- 10mg
- Price
- $144
- Updated
- 2021/12/16
- Product number
- 1798CT
- Product name
- 2-(5-Fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline
- Packaging
- 10mg
- Price
- $232
- Updated
- 2021/12/16
- Product number
- CS-5226
- Product name
- APTO-253
- Purity
- 98.15%
- Packaging
- 50mg
- Price
- $456
- Updated
- 2021/12/16
- Product number
- BA166663
- Product name
- APTO 253
- Packaging
- 50mg
- Price
- $472.5
- Updated
- 2021/12/16
LOR 253 Chemical Properties,Usage,Production
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
LOR 253 Preparation Products And Raw materials
Raw materials
Preparation Products
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