LC 2

Pricing Availability   Qty
说明: Selective KRAS Degrader (PROTAC®)
化学名: (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
纯度: ≥95% (HPLC)
说明书
引用文献
评论
文献 (3)

生物活性 for LC 2

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.

技术数据 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
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.

溶解性数据 for LC 2

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 113.28 100

制备储备液 for LC 2

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for LC 2

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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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.

Targeted Protein Degradation Poster

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