Cas No.: | 2016795-77-8 |
Chemical Name: | EC330 |
Synonyms: | EC330;EC-330; EC 330;Estra-4,9-dien-3-one, 11-(4-cyclopropylphenyl)-17-(1,1-difluoro-2-propyn-1-yl)-17-hydroxy-, (11β,17β)- |
SMILES: | FC(C#C[H])([C@@]1(C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4=C([H])C(C([H])([H])C([H])([H])C4=C3[C@@]([H])(C3C([H])=C([H])C(=C([H])C=3[H])C3([H])C([H])([H])C3([H])[H])C([H])([H])[C@@]21C([H])([H])[H])=O)O[H])F |
Formula: | C30H32F2O2 |
M.Wt: | 462.570695877075 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | EC330 is a leukemia inhibitory factor (LIF) inhibitor. |
In Vivo: | 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]. |
In Vitro: | 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]. |
References: | [1]. Nair HB, et al. Discovery and preclinical pharmacology of EC330: A first-in-class leukemia inhibitory factor (LIF) inhibitor |