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Tosedostat (CHR2797)

Catalog No.S1522 1 Product Citation(s)
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Tosedostat (CHR2797) Chemical Structure

  • Ki16425

    Ki16425 is a LPA receptor inhibitor with selectivity for LPA1 (Ki = 0.34 μM)and LPA3(Ki = 0.93 μM)vs. LPA2(Ki = 6.5 µM)

  • LY315920(Varespladib)

    LY315920(Varespladib) is a sPLA2 inhibitor (IC50 of 9.6 ±1 nM)

  • Abiraterone (CB-7598)

    Abiraterone (CB-7598) is a potent steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor with an IC50 at 4 nM.

  • TAK-700 (Orteronel)

    Inhibitor of the 17,20 lyase.

  • Cilostazol

    Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease.

  • Isotretinoin

    It was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.

  • Trilostane

    Trilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.

  • Sildenafil citrate

    Sildenafil citrate is an agent used to treat erectile dysfunction and pulmonary arterial hypertension (PAH).

  • Voriconazole

    Voriconazole (VFEND) is a triazole antifungal medication that is generally used to treat serious, invasive fungal infections.

  • Cilomilast (SB-207499)

    Cilomilast (SB-207499) is among the first of a new generation of PDE4 inhibitors (Ki ≈100 nM).

Biological Activity

Tosedostat (CHR2797) is an aminopeptidase inhibitor with IC50 of 100, 150, 220, >1000, >5000, >10000 and >30000 nM for LAP, PuSA, aminopeptidase N, aminopeptidase B, PILSAP, LTA4 hydrolase and MetAP2, respectively.
It has demonstrated anti-tumour activity in a number of models of cancer, both as a single agent and in synergy with cytotoxic agents such as carboplatin and paclitaxel. [1][2]

References on Tosedostat (CHR2797)
  • [1] Cancer Res 2008;68:6669-6679
  • [2] Clin Cancer Res 2009;15:4978-4985
Molecular Weight (WM): 406.47
Formula:

C21H30N2O6

CAS No.: 238750-77-1
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥81mg/mL 
Water <1mg/mL 
Ethanol ≥81mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

View current batch:
COA H-NMR HPLC

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Recommended Screening Libraries

Selleck's high quality products have been used in several published research findings, including the following:

Host proteasomal degradation generates amino acids essential for intracellular bacterial growth.

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