LC 2
Tocris Bioscience, part of Bio-Techne | Catalog # 7420
Selective KRAS Degrader (PROTAC®)
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- De Vita The missing link between (un)druggable and degradable KRAS. ACS Cent.Sci. 2020 PMID: 32875070
- Bond Targeted degradation of oncogenic KRAS G12C by VHL-recruiting PROTACs. ACS Cent.Sci. 2020 PMID: 32875077
Product Specific Notices for LC 2
For research use only
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