| Identification | Back Directory | [Name]
3-[3-[(2S)-2-[[[7-(8-chloro-1-naphthalenyl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoro-1-oxo-2-propen-1-yl)-1-piperazinyl]-5,6,7,8 | [CAS]
2561529-98-2 | [Synonyms]
MRTX849 ethoxypropanoic acid
3-[3-[(2S)-2-[[[7-(8-chloro-1-naphthalenyl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoro-1-oxo-2-propen-1-yl)-1-piperazinyl]-5,6,7,8
Propanoic acid, 3-[3-[(2S)-2-[[[7-(8-chloro-1-naphthalenyl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoro-1-oxo-2-propen-1-yl)-1-piperazinyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl]oxy]methyl]-1-pyrrolidinyl]propoxy]- | [Molecular Formula]
C37H43ClFN7O5 | [MDL Number]
MFCD34567052 | [MOL File]
2561529-98-2.mol | [Molecular Weight]
720.23 |
| Hazard Information | Back Directory | [Uses]
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (IC50s between 0.25 and 0.76 μM)[1][2]. | [IC 50]
KRas G12C | [References]
[1] Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375. DOI:10.1021/acscentsci.0c00411
[2] De Vita E, et al. The Missing Link between (Un)druggable and Degradable KRAS. ACS Cent Sci. 2020;6(8):1281-1284. DOI:10.1021/acscentsci.0c00920 |
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