Cas No.: | 2012591-09-0 |
Chemical Name: | (8S,11R,13S,14S,17S)-17-(1,1-difluoroprop-2-yn-1-yl)-17-hydroxy-13-methyl-11-(2',4',6'-trimethyl-[1,1'-biphenyl]-4-yl)-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one |
Synonyms: | EC359 |
SMILES: | C1C2C(CC[C@]([H])3C=2[C@H](C2=CC=C(C4=C(C)C=C(C)C=C4C)C=C2)C[C@@](C)2[C@]3([H])CC[C@@]2(C(F)(F)C#C)O)=CC(=O)C1 |
Formula: | C36H38F2O2 |
M.Wt: | 571.715 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | EC-359 (EC359) is a first-in-class, orally available inhibitor of leukemia inhibitory factor (LIF), blocks LIF-LIFR interaction and binds to LIFR with affinity of 81 nM in SPR assay; displays limited binding to classical steroid receptors; shows cytoskeletal disruption and targeting cancer-associated fibroblasts (CAFs) through inhibition of alpha-SMA but not beta-tubulin, reduces the STAT3 phosphorylation, mTOR and further downstream signaling cascades; dose dependently reduces tumor burden in both TNBC xenograft and murine syngeneic MM51 models (1 and 5 mg/kg dose). |