5428-80-8 Usage
Description
[2-(4-chlorophenyl)quinolin-4-yl]-(2-piperidyl)methanol, also known as Vacquinol-1, is a member of the vacquinol class of quinine derivatives. It is a novel compound that specifically targets and stimulates the death of glioblastoma cells, a type of aggressive brain cancer, through a unique mechanism involving massive macropinocytotic vacuolization, ATP depletion, and cytoplasmic membrane rupture. A key effector of Vacquinol-1 is MAPK kinase 4 (MKK4), making it an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells. It has demonstrated the ability to induce ATP depletion in glioblastoma cells without affecting other cell types such as fibroblasts, embryonic stem cells, or osteosarcoma cells. Vacquinol-1 also exhibits oral bioavailability, good brain penetrance, and excellent pharmacokinetics.
Uses
Used in Anticancer Applications:
[2-(4-chlorophenyl)quinolin-4-yl]-(2-piperidyl)methanol is used as an anticancer agent specifically targeting glioblastoma cells. Its application is based on its ability to induce massive macropinocytotic vacuolization, ATP depletion, and cytoplasmic membrane rupture in these cancer cells, leading to cell death. This selective toxicity makes Vacquinol-1 a promising candidate for the treatment of glioblastoma, a highly aggressive and difficult-to-treat form of brain cancer.
Used in Pharmaceutical Research:
Vacquinol-1 is used as a research tool in the development of novel cancer therapies. Its unique mechanism of action and selectivity for glioblastoma cells make it an attractive compound for studying the underlying pathways and potential therapeutic strategies against this devastating disease.
Used in Drug Delivery Systems:
In the context of drug delivery, [2-(4-chlorophenyl)quinolin-4-yl]-(2-piperidyl)methanol can be used to improve the targeting and efficacy of glioblastoma treatments. Its good brain penetrance and pharmacokinetic properties suggest that it could be a valuable component in the design of drug delivery systems specifically aimed at treating brain cancers.
Used in Preclinical Studies:
Vacquinol-1 is used in preclinical studies to evaluate its potential as a therapeutic agent for glioblastoma. Oral administration of Vacquinol-1 has been shown to substantially impair the growth of engrafted glioblastoma cell tumors in mice and prolong survival, indicating its potential for further development and testing in clinical settings.
Used in Application Industry:
[2-(4-chlorophenyl)quinolin-4-yl]-(2-piperidyl)methanol is used in the pharmaceutical and biotechnology industries for the development of novel cancer therapies, specifically for the treatment of glioblastoma. Its unique properties and mechanisms of action make it a valuable compound for research and development efforts in these fields.
Check Digit Verification of cas no
The CAS Registry Mumber 5428-80-8 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 5,4,2 and 8 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 5428-80:
(6*5)+(5*4)+(4*2)+(3*8)+(2*8)+(1*0)=98
98 % 10 = 8
So 5428-80-8 is a valid CAS Registry Number.
InChI:InChI=1/C21H21ClN2O/c22-15-10-8-14(9-11-15)20-13-17(16-5-1-2-6-18(16)24-20)21(25)19-7-3-4-12-23-19/h1-2,5-6,8-11,13,19,21,23,25H,3-4,7,12H2
5428-80-8Relevant articles and documents
COMPOUNDS AND USE FOR TREATING CANCER
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, (2016/08/17)
The present invention relates to certain 2,4-disubstituted quinoline derivatives, to their therapy, as well as to pharmaceutical compositions comprising said compounds. More specifically the invention relates to certain 2,4-disubstituted quinoline derivatives or pharmaceutical compositions comprising said compounds for the treatment of cancers characterized by overactive Ras and/or Rac or signalling pathway.
