主页 / 药理学 / Enzymes / Hydrolases / Glutaminase / Glutaminase Inhibitors / CB 839

CB 839

Cat. No. 7591 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 glutaminase GLS1 inhibitor
化学名： N-[5-[4-[6-[[2-[3-(Trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-2-pyridineacetamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论
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 CB 839

CB 839 is a potent non-competitive glutaminase (GLS1) inhibitor (IC50 = 24 nM for recombinant human GAC). The compound exhibits selectivity for GLS1 over GLS2. CB 839 displays antiproliferative activity in a triple-negative breast cancer cell line (GI50 values are 19 and 55 nM against MDA-MB-231 and HCC1806, respectively); it reduces glutamine consumption and glutamate production rates in HCC1806 cells. CB 839 displays significant antitumor activity as a single agent in a patient-derived TNBC xenografts model. CB 839 inhibits the growth of basal-like HER2 cell line JIMT-1 xenografts in mice, both as a single agent and in combination with Paclitaxel (Cat. No. 1097). CB 839 works with Erlotinib (Cat. No. 7194) to reduce glucose and glutamine uptake, increase energetic stress and activate the AMP-activated protein kinase (AMPK) pathway in EGFR (del19) non-small cell lung cancer xenografts in vivo. CB 839 is orally bioavailable.

技术数据 for CB 839

分子量 571.58
公式 C26H24F3N7O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1439399-58-2
PubChem ID 71577426
InChI Key PRAAPINBUWJLGA-UHFFFAOYSA-N
Smiles O=C(NC1=NN=C(CCCCC2=NN=C(NC(CC3=CC=CC(OC(F)(F)F)=C3)=O)C=C2)S1)CC4=NC=CC=C4

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 CB 839

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 57.16 100

制备储备液 for CB 839

以下数据基于产品分子量 571.58。 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 1.75 mL 8.75 mL 17.5 mL
5 mM 0.35 mL 1.75 mL 3.5 mL
10 mM 0.17 mL 0.87 mL 1.75 mL
50 mM 0.03 mL 0.17 mL 0.35 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 CB 839

参考文献是支持产品生物活性的出版物。

Gross et al (2014) Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol.Cancer Ther. 13 890 PMID: 24523301

Jacque et al (2015) Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition. Blood 126 1346 PMID: 26186940

Matre et al (2016) Inhibiting glutaminase in acute myeloid leukemia: metabolic dependency of selected AML subtypes. Oncotarget 7 79722 PMID: 27806325

Momcilovic et al (2017) Targeted inhibition of EGFR and glutaminase induces metabolic crisis in EGFR mutant lung cancer. Cell Rep. 18 601 PMID: 28099841

Biancur et al (2017) Compensatory metabolic networks in pancreatic cancers upon perturbation of glutamine metabolism. Nat.Commun. 8 15965 PMID: 28671190

Zhou et al (2019) Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun.Signal. 17 99 PMID: 31429768

If you know of a relevant reference for CB 839, 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 Glutaminase Inhibitors

关键词: CB 839, CB 839 supplier, CB839, potent, inhibits, orally, bioavailable, antitumor, non-competitive, inhibitors, glutaminases, GLS1, paclitaxel, erlotinib, antiproliferative, Glutaminase, 7591, Tocris Bioscience

篇 CB 839 的引用文献

引用文献是使用了 Tocris 产品的出版物。

目前没有 CB 839 的引用文献。 您是否知道使用了 Tocris CB 839 的优秀论文？ 请告知我们.

CB 839 的评论

目前没有该产品的评论。 Be the first to review CB 839 and earn rewards!

Have you used CB 839?

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。

Cancer Metabolism Research Product Guide

Cancer Metabolism Research Product Guide

This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:

Cancer Metabolism Poster

Cancer Metabolism Poster

This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.