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Submit ReviewLC 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.
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 |
分子量 | 1132.8 |
公式 | C59H71ClFN11O7S |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 113.28 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: LC 2, LC 2 supplier, LC2, PROTACs, targeted, protein, degraders, degradation, von, Hippel, Lindau, E3, ligase, KRAS, ERK, selective, VHL, MRTX849, Ras, GTPases, Raf, and, Degraders, 7420, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.
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