EC359 | LIFR inhibitor | Probechem Biochemicals

Chemical Structure : EC359

CAS No.: 2012591-09-0

EC359 (EC-359)

Catalog No.: PC-35333Not For Human Use, Lab Use Only.

EC359 (EC-359) 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.

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5 mg	$258	In stock
10 mg	$398	In stock
25 mg	$588	In stock
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Biological Activity

EC359 (EC-359) 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.
EC-359 displays limited binding to classical steroid receptors.
EC-359 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.
EC-359 dose dependently reduces tumor burden in both TNBC xenograft and murine syngeneic MM51 models (1 and 5 mg/kg dose).

Physicochemical Properties

M.Wt	571.715
Formula	C36H38F2O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

References

1. Hareesh B. Nair, et al. Abstract LB-B04: Development of a first-in-class leukemia inhibitory factor (LIF)/LIFR inhibitor, EC359 for targeted therapy

EC359 (EC-359)

Biological Activity

Physicochemical Properties

References

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