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| 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)- Basic information |
Product 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)- | Synonyms: | 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)-;GNE-502 | CAS: | 1953134-16-1 | MF: | C25H30FN3O3S | MW: | 471.59 | EINECS: | | Product Categories: | | Mol File: | 1953134-16-1.mol | |
| 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)- Chemical Properties |
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 |
| 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)- Usage And Synthesis |
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. |
| 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)- Preparation Products And Raw materials |
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Tag: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)-(1953134-16-1)
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