LC 2

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Cat.No. 7420 - LC 2 | C59H71ClFN11O7S | CAS No. 2502156-03-6
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)
Datasheet
Citations
Reviews
Literature (4)

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

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.

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

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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.

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!

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