LC 2 is a mutant-selective PROTAC® Degrader of KRAS, comprising a ligand for the von Hippel Lindau E3 ligase joined to the KRAS inhibitor MRTX849. LC 2 induces selective degradation of KRASG12C in cancer cell lines without inducing degradation of any other mutants (DC50 = 0.25-0.76 μM), leading to suppression of MAPK signaling and modulation of ERK signaling in both homozygous and heterozygous KRASG12C cancer cell lines. LC 2 inhibits phosphorylation of ERK in SW1573 cell lines.
MedKoo Cat#: 465593
Name: LC 2
CAS#: 2502156-03-6
Chemical Formula: C59H71ClFN11O7S
Exact Mass: 1131.4931
Molecular Weight: 1132.80
Elemental Analysis: C, 62.56; H, 6.32; Cl, 3.13; F, 1.68; N, 13.60; O, 9.89; S, 2.83
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 113.3 | 100.00 |
The following data is based on the product molecular weight 1,132.80 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
