LC-2

• Description :

  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].

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  PROTACs; Ras

• 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/protac-krasg12c-degrader-lc-2.html

• Purity :

  98.48

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  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

• Molecular Formula :

  C59H71ClFN11O7S

• Molecular Weight :

  1132.78

• Precautions :

  H302, H315, H319, H335

• References & Citations :

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

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  K-Ras; von Hippel-Lindau (VHL)

• CAS Number :

  [2502156-03-6]