主页 / Product Type / PROTAC® Degraders & Targeted Protein Degradation / Protein Degraders / Raf and Ras Degraders / CG 858

CG 858

Cat. No. 7427 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
Pricing Availability   Qty
说明： Selective BRAF-V600E protein Degrader (uSMITE™)
化学名： N-[[4-[3-[2,6-Difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]pentanamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论
文献 (3)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for CG 858

CG 858 is a selective BRAF-V600E protein Degrader (uSMITE™). CG 858 comprises the BRAF kinase inhibitor vemurafenib linked to the E3 ligase ligand Thalidomide (Cat. No. 0652). CG 858 dose-dependently degrades BRAF-V600E but not wild type BRAF, and reduces cell viability and colony formation in HT-29 and A375 cells (DC50 values are 124 nM and 500 nM, respectively). Exhibits 88% degradation at 500 nM. CG 858 also impairs melanoma cell growth.

CG 858 negative control (Cat. No. 7428) and B-Raf antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3424.

许可信息

Sold under license from Cullgen.

技术数据 for CG 858

分子量 839.87
公式 C42H39F2N7O8S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2417296-82-1
PubChem ID 155551346
InChI Key AAIPPJPUZKZIHC-UHFFFAOYSA-N
Smiles CCCS(=O)(NC1=CC=C(C(C(C2=CNC3=NC=C(C4=CC=C(C=C4)CNC(CCCCNC5=CC=C6C(N(C(C6=C5)=O)C7CCC(NC7=O)=O)=O)=O)C=C23)=O)=C1F)F)=O

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 CG 858

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 83.99 100

制备储备液 for CG 858

以下数据基于产品分子量 839.87。 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 1.19 mL 5.95 mL 11.91 mL
5 mM 0.24 mL 1.19 mL 2.38 mL
10 mM 0.12 mL 0.6 mL 1.19 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

参考文献 for CG 858

参考文献是支持产品生物活性的出版物。

Han et al (2020) Discovery of selective small molecule degraders of BRAF-V600E. J.Med.Chem. 63 4069 PMID: 32223235

If you know of a relevant reference for CG 858, please let us know.

按标靶查看相关产品

关键词: CG 858, CG 858 supplier, CG858, degraders, targeted, protein, degradation, degrades, E3, ligase, uSMITE, BRAF-V600E, kinase, Ubiquitin-mediated, Small, Molecule-Induced, Target, Elimination, PROTAC, Raf, Kinase, Degraders, and, Ras, 7427, Tocris Bioscience

篇 CG 858 的引用文献

引用文献是使用了 Tocris 产品的出版物。

目前没有 CG 858 的引用文献。 您是否知道使用了 Tocris CG 858 的优秀论文？ 请告知我们.

CG 858 的评论

目前没有该产品的评论。 Be the first to review CG 858 and earn rewards!

Have you used CG 858?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

该领域的文献

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。

TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
RAS Oncoproteins Scientific Review

RAS Oncoproteins Scientific Review

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