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LC-2 is a potent first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.
| Molecular Weight | 1132.78 |
| Formula | C59H71ClFN11O7S |
| CAS Number | 2502156-03-6 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Elena De Vita, et al. ACS Cent Sci. The Missing Link between (Un)dгυggаbΙе and Degradable KRAS
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