GLL398

Overview
Catalog #	bs-7024c-10mg-solid
Product Name	GLL398
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 398.26 Formula: C25 H23 B O4 CAS Number: 2077980-83-5 InChi Key: BINZFDGAOTWQNC-YGCRUXFTSA-N InChi: InChI=1S/C25H23BO4/c1-2-23(19-6-4-3-5-7-19)25(21-13-15-22(16-14-21)26(29)30)20-11-8-18(9-12-20)10-17-24(27)28/h3-17,29-30H,2H2,1H3,(H,27,28)/b17-10+,25-23+ Smiles: CCC(=C(C1C=CC(C=CC(O)=O)=CC=1)C1C=CC(=CC=1)B(O)O)C1C=CC=CC=1 Purity: 98.0 Solubility: Soluble in DMSO Appearance: Solid Power. Shelf Life: 1.0 years
Description	GLL398 is an Oral Selective Estrogen Receptor Downregulator. GLL398 strongly binds to ERα in a fluorescence resonance energy transfer binding assay (IC50 =1.14 nM) and potently degrades ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). Most importantly, the introduction of the boronic acid group confers superior oral bioavailability of GLL398 (AUC = 36.9 μg·h/mL) in rats as compared to GW7604 (AUC = 3.35 μg·h/mL). The strikingly favorable pharmacokinetic property of GLL398 makes it a promising oral SERD suitable for clinical evaluation.