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LC 2

Catalog #: 7420 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7420/2
LC 2 | CAS No. 2502156-03-6 | Active Degraders
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Description: Selective KRAS Degrader (PROTAC®)

Chemical Name: (2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-Chloronaphthalen-1-yl)-4-((S)-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-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Purity: ≥95%

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Biological Activity

LC 2 is a mutant-selective KRAS Degrader (PROTAC®), 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.

Technical Data

E3 ligase
VHL
DC50 / Dmax
250 nM (90%) - Degradation of KRASG12C in NCI-H23 cells after 24 h treatment
Selectivity confirmed by global proteomics
No
M.Wt:
1132.8
Formula:
C59H71ClFN11O7S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥95%
Storage:
Store at -20°C
CAS No:
2502156-03-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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