CHR 2797

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Description: Aminopeptidase inhibitor
Alternative Names: Tosedostat
Chemical Name: α-[[(2R)-2-[(1S)-1-Hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]amino]-benzeneacetic acid cyclopently ester
Purity: ≥98% (HPLC)
Citations (3)

Biological Activity for CHR 2797

CHR 2797 is an aminopeptidase inhibitor (IC50 values are 100, 150, 220, > 1000, > 5000, > 10000 and > 30000 nM for LAP, PuSA, aminopeptidase N, aminopeptidase B, PILSAP, LTA4 hydrolase and MetAP2, respectively). Potently inhibits tumor cell proliferation in a variety of tumor cell lines in vitro and in vivo. Also inhibits neprilysin (IC50 = 900 nM). Exhibits antinociceptive activity and enhances the efficacy of Morphine (Cat. No. 5158) in the hot-plate and tail-flick assays, via an action on the peripheral nervous system.

Compound Libraries for CHR 2797

CHR 2797 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for CHR 2797

M. Wt 406.48
Formula C21H30N2O6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 238750-77-1
PubChem ID 15547703
Smiles O=C([C@H]([C@]2=CC=CC=C2)NC([C@@H]([C@@H](C(NO)=O)O)CC(C)C)=O)OC1CCCC1

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CHR 2797

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 40.65 100
ethanol 20.32 50

Preparing Stock Solutions for CHR 2797

The following data is based on the product molecular weight 406.48. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.46 mL 12.3 mL 24.6 mL
5 mM 0.49 mL 2.46 mL 4.92 mL
10 mM 0.25 mL 1.23 mL 2.46 mL
50 mM 0.05 mL 0.25 mL 0.49 mL

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Product Datasheets for CHR 2797

Certificate of Analysis / Product Datasheet
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References for CHR 2797

References are publications that support the biological activity of the product.

Krige et al (2008) CHR-2797: an anitproliferative aminopeptidase inhibitor that leads to amino acid deprivation in human leukemic cells. Cancer Res. 68 6669 PMID: 18701491

Moore et al (2009) Aminopeptidase inhibition as a targeted treatment strategy in myeloma. Mol.Cancer Ther. 8 762 PMID: 19372548

Singh et al (2019) Discovery of anticancer clinical candidate, Tosedostat, as an analgesic agent. ACS Chem.Neurosci. 10 4007 PMID: 31415151

If you know of a relevant reference for CHR 2797, please let us know.

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Keywords: CHR 2797, CHR 2797 supplier, aminopeptidases, inhibitors, inhibits, proteases, proteinases, CHR2797, neprilysin, neutral, endopeptidase, NEP, Tosedostat, Aminopeptidases, 3595, Tocris Bioscience

3 Citations for CHR 2797

Citations are publications that use Tocris products. Selected citations for CHR 2797 include:

Orth-He et al (2023) Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation. Cell Rep 42 111965 PMID: 36649711

Yogin et al (2022) Cancer genes disfavoring T cell immunity identified via integrated systems approach. Cell Rep 40 111153 PMID: 35926468

Justin R et al (2022) M24B aminopeptidase inhibitors selectively activate the CARD8 inflammasome. Nat Chem Biol 18 565-574 PMID: 35165443

Do you know of a great paper that uses CHR 2797 from Tocris? Please let us know.

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