968

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Cat.No. 5460 - 968 | C27H27BrN2O | CAS No. 311795-38-7
Description: Allosteric inhibitor of glutaminase
Chemical Name: 5-[3-Bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethylbenzo[a]phenanthridin-4(1H)-one
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Allosteric inhibitor of glutaminase. Blocks Rho-GTPase-dependent transformation of fibroblasts. Suppresses breast cancer cell growth and invasive activity in vitro. Also inhibits P-493 B lymphoma cell growth and reduces tumor size of P-493 cell xenografts in mice.

Technical Data

M. Wt 475.42
Formula C27H27BrN2O
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 311795-38-7
PubChem ID 3099980
InChI Key NVFRRJQWRZFDLM-UHFFFAOYSA-N
Smiles BrC1=CC(C(C5=C4CC(C)(C)CC5=O)NC3=C4C2=CC=CC=C2C=C3)=CC=C1N(C)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 9.51 20

Preparing Stock Solutions

The following data is based on the product molecular weight 475.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.1 mL 10.52 mL 21.03 mL
5 mM 0.42 mL 2.1 mL 4.21 mL
10 mM 0.21 mL 1.05 mL 2.1 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

Wang et al (2010) Targeting mitochondrial glutaminase activity inhibits oncogenic transformation. Cancer Cell 18 207 PMID: 20832749

Stalnecker et al (2015) Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells. Proc.Natl.Acad.Sci.U.S.A. 112 394 PMID: 25548170

Lu et al (2010) Cancer metabolism: is glutamine sweeter than glucose? Cancer Cell 18 199 PMID: 20832746


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Keywords: 968, supplier, Hydrolases, allosteric, inhibitors, inhibits, glutaminase, oncogene, transformation, gls1, Glutaminase, Glutaminase, Tocris Bioscience

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

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