LC 2

Tocris Bioscience | Catalog # 7420

Selective KRAS Degrader (PROTAC®)
Tocris Bioscience

Key Product Details

Description

Selective KRAS Degrader (PROTAC®)
View all Active Degraders »

Product Description

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.

Product Specifications for LC 2

Molecular Weight

1132.80

Formula

C59H71ClFN11O7S

Storage

Store at -20°C

Purity

≥95% (HPLC)

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

CAS Number

2502156-03-6

PubChem ID

154727765

InChI Key

ZCGQZLKPUVGCBQ-HLMPTVQRSA-N

SMILES

CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCOCCCN4CCC[C@H]4COC5=NC(N6CCN(C(C(F)=C)=O)[C@H](C6)CC#N)=C7CCN(C8=CC=CC9=C8C(Cl)=CC=C9)CC7=N5)=O)=O)O)=O)SC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 113.28 100

Preparing Stock Solutions for LC 2

The following data is based on the product molecular weight 1132.80.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.88 mL 4.41 mL 8.83 mL
5 mM 0.18 mL 0.88 mL 1.77 mL
10 mM 0.09 mL 0.44 mL 0.88 mL
50 mM 0.02 mL 0.09 mL 0.18 mL

Calculators

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Background References

References are publications that support the biological activity of the product.

Product Documents for LC 2

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for LC 2

For research use only

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