| Chemical Properties | Back Directory | [Boiling point ]
659.3±55.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 125 mg/mL (231.19 mM) | [form ]
Solid | [pka]
12.89±0.60(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor which directly interacts with LIFR to effectively block LIF/LIFR interactions. | [Uses]
EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions[1]. EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [in vivo]
EC359 (5 mg/kg; subcutaneous injection; 3 days per week; for 25 days; female athymic nude mice) treatment significantly reduces the tumor progression. The body weights of mice in EC359-treated groups remains unchanged confirming the low toxicity of EC359[1]. | Animal Model: | 8-week-old female athymic nude mice with MDA-MB-231 cells[1] | | Dosage: | 5 mg/kg | | Administration: |
Subcutaneous injection; 3 days per week; for 25 days | | Result: | Significantly reduced the tumor progression.
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| [References]
[1] Viswanadhapalli S, et al. EC359: A First-in-Class Small-Molecule Inhibitor for Targeting Oncogenic LIFR Signaling in Triple-Negative Breast Cancer. Mol Cancer Ther. 2019 Aug;18(8):1341-1354. DOI:10.1158/1535-7163.MCT-18-1258 |
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