bs-7024C
[Life Science]
GLL398
DATASHEET
Formulation Powder
Storage: Store in dry, dark place at -20C for 1 year.
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
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.
Size: 10mg solid,2mg solid 10mg solid,2mg solid
Applications: Life Science()
For research use only. Not intended for diagnostic or therapeutic use.