主页 / 药理学 / Enzymes / Proteases / Proteasome / Proteasome Inhibitors / Carfilzomib

Carfilzomib

Cat. No. 7188 1 条评论 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： Potent irreversible proteasome inhibitor; active in vivo
别名： PR-171
化学名： (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论 (1)
文献 (2)
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 Carfilzomib

Carfilzomib is a potent irreversible proteasome inhibitor. Preferentially inhibits the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM) in vitro with minimal cross-reactivity to other proteases. Exhibits little or no effect on PGPH and T-L activities. Activates prosurvival autophagy and induces cell apoptosis. Acts synergistically with dexamethasone (Cat. No. 1126). Suppresses tumor growth in an in vivo xenograft model. Decreases bone resorption and enhances bone formation in non-tumor bearing mice.

技术数据 for Carfilzomib

分子量 719.92
公式 C40H57N5O7
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 868540-17-4
PubChem ID 11556711
InChI Key BLMPQMFVWMYDKT-NZTKNTHTSA-N
Smiles CC(C)C[C@H](NC(=O)[C@H](CCC1=CC=CC=C1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1

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 Carfilzomib

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 71.99 100
ethanol 14.4 20

制备储备液 for Carfilzomib

以下数据基于产品分子量 719.92。 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 1.39 mL 6.95 mL 13.89 mL
5 mM 0.28 mL 1.39 mL 2.78 mL
10 mM 0.14 mL 0.69 mL 1.39 mL
50 mM 0.03 mL 0.14 mL 0.28 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 Carfilzomib

参考文献是支持产品生物活性的出版物。

Demo et al (2007) Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. Cancer Res. 67 6383 PMID: 17616698

Zhou et al (2009) Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J.Med.Chem. 52 3028 PMID: 19348473

Dou et al (2014) Overview of proteasome inhibitor-based anti-cancer therapies: perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system. Curr.Cancer Drug Targets 14 517 PMID: 25092212

Wang et al (2020) Fast identification of possible drug treatment of coronavirus disease-19 (COVID-19) through computational drug repurposing study. J.Chem.Inf.Model 60 3277 PMID: 32315171

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

按标靶查看相关产品

按产品操作查看相关产品

查看全部 Proteasome Inhibitors

关键词: Carfilzomib, Carfilzomib supplier, Potent, irreversible, proteasome, inhibitor, inhibitors, inhibits, inhibit, active, in, vivo, 20S, proteasomes, 20Si, PR-171, Proteasome, 7188, Tocris Bioscience

篇 Carfilzomib 的引用文献

引用文献是使用了 Tocris 产品的出版物。

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

Carfilzomib 的评论

平均评分: 5 (Based on 1 Review.)

5 星
100%
4 星
0%
3 星
0%
2 星
0%
1 星
0%

Have you used Carfilzomib?

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

Filter by:


Apoptosis induction.
By MARINA KOUTSIOUMPA on 10/13/2022
分析类型： In Vitro
种属： Human

Combinatorial treatments of carfilzomib with chemotherapeutics led to synergistic apoptotic phenotype in vitro.

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
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