MRTX849 ethoxypropanoic acid

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].

Product Specifications

CAS Number

[2561529-98-2]

UNSPSC

12352005

Target

Ras; Target Protein Ligand-Linker Conjugates

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mrtx849-ethoxypropanoic-acid.html

Solubility

10 mM in DMSO

Smiles

O=C(N1CCN(C2=C3CCN(CC3=NC(OC[C@@H]4CCCN4CCCOCCC(O)=O)=N2)C5=CC=CC6=C5C(Cl)=CC=C6)C[C@@H]1CC#N)C(F)=C

Molecular Formula

C37H43ClFN7O5

Molecular Weight

720.23

References & Citations

[1]Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6 (8) :1367-1375.|[2]De Vita E, et al. The Missing Link between (Un) druggable and Degradable KRAS. ACS Cent Sci. 2020;6 (8) :1281-1284.