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Description: Selective KRAS 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% (HPLC)
Biological Activity for LC 2
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.
Technical Data for LC 2
| 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 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for LC 2
| 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 1132.8. 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 | 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 |
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Product Datasheets for LC 2
References for LC 2
References are publications that support the biological activity of the product.
Bond et al (2020) Targeted degradation of oncogenic KRAS G12C by VHL-recruiting PROTACs. ACS Cent.Sci. 6 1367 PMID: 32875077
De Vita et al (2020) The missing link between (un)druggable and degradable KRAS. ACS Cent.Sci. 6 1281 PMID: 32875070
If you know of a relevant reference for LC 2, please let us know.
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Keywords: LC 2, LC 2 supplier, LC2, PROTACs, targeted, protein, degraders, degradation, von, Hippel, Lindau, E3, ligase, KRAS, ERK, selective, VHL, MRTX849, Active, Degraders, Ras, GTPases, 7420, Tocris Bioscience
Citations for LC 2
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia