For research use only. Not for therapeutic Use.
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer[1].
GNE-502 (10 and 100 mg/kg; p.o.) possesses sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model[1].
GNE-502 shows dose dependent tumor growth inhibition at 10 mg/kg and 30 mg/kg, with tumor stasis at 100 mg/kg[1].
| Catalog Number | I045389 |
| CAS Number | 1953134-16-1 |
| Synonyms | (1R,3R)-1-[4-[2-[3-(fluoromethyl)azetidin-1-yl]ethoxy]phenyl]-3-methyl-2-methylsulfonyl-1,3,4,9-tetrahydropyrido[3,4-b]indole |
| Molecular Formula | C25H30FN3O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C25H30FN3O3S/c1-17-13-22-21-5-3-4-6-23(21)27-24(22)25(29(17)33(2,30)31)19-7-9-20(10-8-19)32-12-11-28-15-18(14-26)16-28/h3-10,17-18,25,27H,11-16H2,1-2H3/t17-,25-/m1/s1 |
| InChIKey | ALLRPIPLWLLBGX-CRICUBBOSA-N |
| SMILES | CC1CC2=C(C(N1S(=O)(=O)C)C3=CC=C(C=C3)OCCN4CC(C4)CF)NC5=CC=CC=C25 |
| Reference | [1]. Zbieg JR, et al. Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer [published online ahead of print, 2021 Aug 20]. Bioorg Med Chem Lett. 2021;128335. |
