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[CAS NO. 916151-99-0] APTO-253
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-16291 |
| Brand: | MCE |
| CAS: | 916151-99-0 |
Overview
| MDL | MFCD25976826 |
|---|---|
| Molecular Weight | 367.38 |
| Molecular Formula | C22H14FN5 |
| SMILES | CC(N1)=C(C(N2)=NC3=C2C4=CC=CN=C4C5=NC=CC=C53)C6=C1C=CC(F)=C6 |
8 Publications Citing Use of MCE
Summary
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 Vitro
APTO-253 (LOR-253) is an inducer of KLF4. APTO-253 (5 μM) induces KLF4 expression, and enhances apoptosis induced by NSC 119875 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 IC
50
s 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 IC
50
s 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02267863 | Aptose Biosciences Inc. |
Acute Myelogenous Leukemia in Relapse|Acute Myelogenous Leukemia, Relapsed, Adult|Acute Myelogenous Leukemia, Adult|Acute Myelogenous Leukemia|High Risk Myelodysplasia
|
October 2014 | Phase 1 |
| NCT01281592 | Aptose Biosciences Inc. |
Advanced or Metastatic Solid Tumours
|
January 2011 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 60 mg/mL ( 163.32 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7220 mL | 13.6099 mL | 27.2198 mL |
| 5 mM | 0.5444 mL | 2.7220 mL | 5.4440 mL |
| 10 mM | 0.2722 mL | 1.3610 mL | 2.7220 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (5.66 mM); Suspended solution; Need ultrasonic
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.
- [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.
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