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Chemical Structure| 13207-66-4 Chemical Structure| 13207-66-4

Structure of 5-Amino-8-hydroxyquinoline
CAS No.: 13207-66-4

Chemical Structure| 13207-66-4

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5A8HQ is a potential proteasome inhibitor with anticancer candidate activity, showing strong proteasome inhibition effects, making it suitable for cancer treatment research.

Synonyms: 5A8HQ

4.5 *For Research Use Only !

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Product Citations

Product Citations

Ingraham, Charles H. IV ; Stalinska, Joanna ; Carson, Sean C. ; Colley, Susan B. ; Rak, Monika ; Lassak, Adam , et al.

Abstract: Glioblastomas are highly aggressive brain tumors for which therapeutic options are very limited. In a quest for new anti-glioblastoma drugs, we focused on specific structural modifications to the benzoyl-phenoxy-acetamide (BPA) structure present in a common lipid-lowering drug, fenofibrate, and in our first prototype glioblastoma drug, PP1. Here, we propose extensive computational analyses to improve the selection of the most effective glioblastoma drug candidates. Initially, over 100 structural BPA variations were analyzed and their physicochemical properties, such as water solubility (- logS), calculated partition coefficient (ClogP), probability for BBB crossing (BBB_SCORE), probability for CNS penetration (CNS-MPO) and calculated cardiotoxicity (hERG), were evaluated. This integrated approach allowed us to select pyridine variants of BPA that show improved BBB penetration, water solubility, and low cardiotoxicity. Herein the top 24 compounds were synthesized and analyzed in cell culture. Six of them demonstrated glioblastoma toxicity with IC50 ranging from 0.59 to 3.24 µM. Importantly, one of the compounds, HR68, accumulated in the brain tumor tissue at 3.7 ± 0.5 µM, which exceeds its glioblastoma IC50 (1.17 µM) by over threefold.

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Product Details of 5-Amino-8-hydroxyquinoline

CAS No. :13207-66-4
Formula : C9H8N2O
M.W : 160.17
SMILES Code : OC1=C2N=CC=CC2=C(N)C=C1
Synonyms :
5A8HQ
MDL No. :MFCD00185837
InChI Key :YDEUKNRKEYICTH-UHFFFAOYSA-N
Pubchem ID :416002

Safety of 5-Amino-8-hydroxyquinoline

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Isoform Comparison

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.24mL

1.25mL

0.62mL

31.22mL

6.24mL

3.12mL

62.43mL

12.49mL

6.24mL

 

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