Tocris Bioscience™ LC 2

Description

Selective KRAS PROTAC™

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.

Negative control LC 2 Epimer (Cat. No. 7421) also available.

PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license.

Specifications

• Chemical Name or Material: (2 S,4 R)-1-(-2-(3-(3-(-2-(((7-(8-Chloronaphthalen-1-yl)-4-(-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-m)
• CAS: 2502156-03-6
• Quantity: 2 mg
• Target: Active Degraders
• Molecular Formula: C₅₉H₇₁ClFN₁₁O₇S
• Purity: 0.95