LC-2 [CAS 2502156-03-6]

LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM[1]. 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[2].

[2502156-03-6]

C59H71ClFN11O7S

1132.78

O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCOCCCN4[C@@H](CCC4)COC5=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C7C(CN(CC7)C8=C9C(Cl)=CC=CC9=CC=C8)=N5)=O)=O

PROTACs; Ras

K-Ras; von Hippel-Lindau (VHL)

98.48

DMSO : 100 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature

H302, H315, H319, H335

H302, H315, H319, H335