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Purity: ≥98%
Etalocib, formerly known as LY293111 and VML295, is a novel diaryl ether carboxylic acid analogue, is a potent and selective inhibitor of the lipoxygenase pathway either directly through 5'-lipoxygenase or via antagonism of the leukotriene B4 (LTB4) receptor. LY293111 has antineoplastic activity in a variety of preclinical models.
| ln Vitro |
The LTB4-induced overexpression of CD11b is inhibited in a concentration-dependent manner by etalocib (LY293111) [1]. Etalocib (LY293111) is a highly effective and specific inhibitor of human neutrophil activity that can be used in vitro [2]. Human pancreatic cancer cells undergo apoptosis and are inhibited from proliferating when exposed to etabacib (LY293111, 250 and 500 nM, 24-72 hours) [3].
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| ln Vivo |
When given intravenously (ED50=14 µg/kg) or orally (ED50=0.4 mg/kg), etalocib (LY293111) produces dose-related inhibition of acute leukotriene B4-induced airway obstruction [2]. Within an hour, A23187-induced pulmonary inflammatory changes can be inhibited by etalocib (LY293111, 10 mg/kg) [2]. In athymic mice, the growth of human pancreatic cancer xenografts is inhibited by etabacib (LY293111, 250 mg/kg/day, oral) [3].
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| Cell Assay |
Cell proliferation assay [3]
Cell Types: MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. [3] Tested Concentrations: 500 nM. Incubation Duration: 24, 48 and 72 hrs (hours). Experimental Results: Concentration-dependent and time-dependent inhibition of thymidine incorporation in MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. Apoptosis analysis [3] Cell Types: MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. Tested Concentrations: 250 and 500 nM. Incubation Duration: 24 hrs (hours). Experimental Results: Apoptosis of human pancreatic cancer cells was induced. |
| Animal Protocol |
Animal/Disease Models: guinea pig[2].
Doses: 1-10 mg/kg. Doses: Take once orally. Experimental Results: A single 1 mg/kg oral dose administered 8 hrs (hrs (hours)) before leukotriene B4 challenge inhibited the increase in isolated lung gas volume by 76.7±7.1% (n=4, P<0.002) and 28.6±20.3% (n= 4, P<0.002). NS) given 24 hrs (hrs (hours)) before challenge. A23187 had no effect on lung air retention 1 hour or 2 hrs (hrs (hours)) after challenge (10 mg/kg). However, at 4 hrs (hrs (hours)), the pulmonary air retention response was Dramatically lower than in vehicle-treated controls and not different from sham. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes within 1 hour but had no effect at 2 or 4 hrs (hrs (hours)) post-challenge. |
| References |
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| Additional Infomation |
LY293111 is an aromatic ether.
Etalocib has been used in trials studying the treatment of Pancreatic Cancer, Carcinoma, Non-Small-Cell Lung, and Unspecified Adult Solid Tumor, Protocol Specific. Etalocib is a second-generation selective leukotriene B4 receptor (LTB4R) antagonist with potential antineoplastic activity. Although the exact underlying mechanism through which LY293111 exerts its effects has not been fully elucidated, this agent selectively binds to and blocks LTB4Rs, thereby inhibiting the downstream signalling pathway. LY29311 has been shown to induce apoptosis and inhibits cellular proliferation in LTB4R expressing cells, such as pancreatic cancer cells. |
| Molecular Formula |
C33H32FNAO6
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|---|---|
| Molecular Weight |
566.59
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| Exact Mass |
544.226
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| CAS # |
161172-51-6
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| Related CAS # |
161172-51-6;
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| PubChem CID |
177941
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
656.8±55.0 °C at 760 mmHg
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| Flash Point |
351.0±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.594
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| LogP |
7.61
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
40
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| Complexity |
743
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GKDIMGQSBSDJNC-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C33H33FO6.Na/c1-3-9-25-29(12-7-13-30(25)40-31-11-6-5-10-26(31)33(36)37)38-18-8-19-39-32-21-28(35)27(20-22(32)4-2)23-14-16-24(34)17-15-23/h5-7,10-17,20-21,35H,3-4,8-9,18-19H2,1-2H3,(H,36,37)/q+1/p-1
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| Chemical Name |
sodium 2-(3-(3-((5-ethyl-4'-fluoro-2-hydroxy-[1,1'-biphenyl]-4-yl)oxy)propoxy)-2-propylphenoxy)benzoate
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| Synonyms |
VML295 VML-295 VML 295 LY293111 LY-293111 LY 293111 PDSP1001237 PDSP2001221 Etalocib
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~183.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.59 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7649 mL | 8.8247 mL | 17.6494 mL | |
| 5 mM | 0.3530 mL | 1.7649 mL | 3.5299 mL | |
| 10 mM | 0.1765 mL | 0.8825 mL | 1.7649 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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