| Identification | Back Directory | [Name]
1H-Pyrido[3,4-b]indole, 1-[4-[2-[3-(fluoromethyl)-1-azetidinyl]ethoxy]phenyl]-2,3,4,9-tetrahydro-3-methyl-2-(methylsulfonyl)-, (1R,3R)- | [CAS]
1953134-16-1 | [Synonyms]
GNE-502
1H-Pyrido[3,4-b]indole, 1-[4-[2-[3-(fluoromethyl)-1-azetidinyl]ethoxy]phenyl]-2,3,4,9-tetrahydro-3-methyl-2-(methylsulfonyl)-, (1R,3R)- | [Molecular Formula]
C25H30FN3O3S | [MOL File]
1953134-16-1.mol | [Molecular Weight]
471.59 |
| Chemical Properties | Back Directory | [Boiling point ]
658.4±65.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [solubility ]
DMSO : 100 mg/mL (212.05 mM; Need ultrasonic) | [form ]
Solid | [pka]
16.75±0.60(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[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. |
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