For research use only. Not for therapeutic Use.
EC330 is a leukemia inhibitory factor (LIF) inhibitor. EC330 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EC330 shows marked specificity in MCF-7 cells overexpressing LIF verses MCF-7 cells. EC330 further shows cytoskeletal disruption and targeting cancer-associated fibroblasts (CAFs) through inhibition of alpha-SMA but not beta-tubulin[1].
EC330 treatment (0.1, 0.5 and 2.5 mg/kg) dose dependently reduces tumor burden in ovarian (IGROV-1) and triple negative breast cancer (MDA-MB-231) cell xenografted mouse models as well as MDA-MB-231 PDX models. EC330 exhibits no reactivity towards thiol-cysteine residues, no off target binding to major receptors, kinases or ion channels. EC330 is orally bioavailable and found to be safe and tolerable in toxicity studies[1].
| Catalog Number | I013672 |
| CAS Number | 2016795-77-8 |
| Synonyms | (8S,11R,13S,14S,17S)-11-(4-cyclopropylphenyl)-17-(1,1-difluoroprop-2-ynyl)-17-hydroxy-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one |
| Molecular Formula | C30H32F2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H32F2O2/c1-3-30(31,32)29(34)15-14-26-24-12-10-21-16-22(33)11-13-23(21)27(24)25(17-28(26,29)2)20-8-6-19(7-9-20)18-4-5-18/h1,6-9,16,18,24-26,34H,4-5,10-15,17H2,2H3/t24-,25+,26-,28-,29-/m0/s1 |
| InChIKey | OWPPSPZDYGHPAN-GCNJZUOMSA-N |
| SMILES | CC12CC(C3=C4CCC(=O)C=C4CCC3C1CCC2(C(C#C)(F)F)O)C5=CC=C(C=C5)C6CC6 |
| Reference | [1]. Nair HB, et al. Discovery and preclinical pharmacology of EC330: A first-in-class leukemia inhibitory factor (LIF) inhibitor |
