YFIZRWPXUYFCSN-UHFFFAOYSA-N
Etalocib
CAS: 161172-51-6
Molecular Formula: C33H33FO6
YFIZRWPXUYFCSN-UHFFFAOYSA-N - Names and Identifiers
| Name | Etalocib |
| Synonyms | VML 295 Etalocib LY293111 LY293111 Exclusive YFIZRWPXUYFCSN-UHFFFAOYSA-N 2-(3-(3-((5-Ethyl-4'-fluoro-2-hydroxy-[1,1'-biphenyl]-4-yl)oxy)propoxy)-2-propylphenoxy)benzoic acid Benzoic acid, 2-[3-[3-[(5-ethyl-4'-fluoro-2-hydroxy[1,1'-biphenyl]-4-yl)oxy]propoxy]-2-propylphenoxy]- |
| CAS | 161172-51-6 |
YFIZRWPXUYFCSN-UHFFFAOYSA-N - Physico-chemical Properties
| Molecular Formula | C33H33FO6 |
| Molar Mass | 544.61 |
| Density | 1?+-.0.06 g/cm3(Predicted) |
| Melting Point | 68-70 °C(Solv: acetonitrile (75-05-8)) |
| Boling Point | 656.8±55.0 °C(Predicted) |
| Solubility | Soluble in DMSO |
| pKa | 3.32±0.36(Predicted) |
| Storage Condition | -20℃ |
| Use | Etalocib, also known as LY293111 and VML295, is a novel diaryl ether carboxylic acid derivative, 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. |
YFIZRWPXUYFCSN-UHFFFAOYSA-N - Reference
| Reference Show more | 1: Saif MW, Oettle H, Vervenne WL, Thomas JP, Spitzer G, Visseren-Grul C, Enas N, Richards DA. Randomized double-blind phase II trial comparing gemcitabine plus LY293111 versus gemcitabine plus placebo in advanced adenocarcinoma of the pancreas. Cancer J. 2009 Jul-Aug;15(4):339-43. PubMed PMID: 19672152. 2: Adrian TE, Hennig R, Friess H, Ding X. The Role of PPARgamma Receptors and Leukotriene B(4) Receptors in Mediating the Effects of LY293111 in Pancreatic Cancer. PPAR Res. 2008;2008:827096. Epub 2009 Jan 27. PubMed PMID: 19190780; PubMed Central PMCID: PMC2631651. 3: Tong WG, Ding XZ, Talamonti MS, Bell RH, Adrian TE. Leukotriene B4 receptor antagonist LY293111 induces S-phase cell cycle arrest and apoptosis in human pancreatic cancer cells. Anticancer Drugs. 2007 Jun;18(5):535-41. PubMed PMID: 17414622. 4: Baetz T, Eisenhauer E, Siu L, MacLean M, Doppler K, Walsh W, Fisher B, Khan AZ, de Alwis DP, Weitzman A, Brail LH, Moore M. A phase I study of oral LY293111 given daily in combination with irinotecan in patients with solid tumours. Invest New Drugs. 2007 Jun;25(3):217-25. Epub 2006 Dec 5. PubMed PMID: 17146732. |
YFIZRWPXUYFCSN-UHFFFAOYSA-N - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.836 ml | 9.181 ml | 18.362 ml |
| 5 mM | 0.367 ml | 1.836 ml | 3.672 ml |
| 10 mM | 0.184 ml | 0.918 ml | 1.836 ml |
| 5 mM | 0.037 ml | 0.184 ml | 0.367 ml |
Last Update：2024-01-02 23:10:35
YFIZRWPXUYFCSN-UHFFFAOYSA-N - Reference Information
| biological activity | Etalocib (LY293111) is an orally active antagonist of the leukotriene (LTB4) receptor, the Ki value for inhibition of [3H]LTB4 binding was 25 nM. Etalocib (LY293111) inhibited ltb4-induced calcium mobilization with an lC50 value of 20 nM. Etalocib (LY293111) can induce apoptosis. |
| Cell Line: | MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. [3] MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. |
| Concentration: | 500 nM. 250 and 500 nM. |
| Incubation Time: | 24, 48, and 72 h. 24 h. |
| Result: | Caused both a concentration-dependent and time-dependent inhibition of thymidine incorporation in both MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. Induced apoptosis in human pancreatic cancer cells. A single 1 mg/kg oral dose inhibited excised lung gas volume increases by 76.7±7.1% (n=4, P<0.002) when given 8 h prior to leukotriene B 4 challenge, and 28.6±20.3% (n=4, NS) when given 24 h before challenge. Had no effect (10 mg/kg) on pulmonary gas trapping at 1 h or 2 h after A23187 challenge. However, at 4 h, the pulmonary gas trapping response was significantly less than that of vehicle-treated controls and not different from sham values. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes at 1 h, but was without effect at 2 h or 4 h after challenge. |
| Animal Model: | Guinea pigs. |
| Dosage: | 1-10 mg/kg. |
| Administration: | Orally once. |
Last Update：2024-04-09 21:32:10
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