Tìm theo
Imexon
Thuốc Gốc
Small Molecule
CAS: 59643-91-3
CTHH: C4H5N3O
PTK: 111.102
Imexon is a substance that is being studied in the treatment of some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma. It belongs to the family of drugs called cyanoaziridine derivatives. Also called Amplimexon. Imexon is a cyanoaziridine derivative. Imexon is a thiol-binding small molecule which induces mitochondrial oxidation, a loss of membrane potential and cytochrome C, leading to apoptosis.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C4H5N3O
Phân tử khối
111.102
Monoisotopic mass
111.043261797
InChI
InChI=1S/C4H5N3O/c5-3-2-1-7(2)4(8)6-3/h2H,1H2,(H2,5,6,8)
InChI Key
InChIKey=BIXBBIPTYBJTRY-UHFFFAOYSA-N
IUPAC Name
4-amino-1,3-diazabicyclo[3.1.0]hex-3-en-2-one
Traditional IUPAC Name
4-amino-1,3-diazabicyclo[3.1.0]hex-3-en-2-one
SMILES
NC1=NC(=O)N2CC12
Độ hòa tan
7.14e+01 g/l
logP
-1.6
logS
-0.19
pKa (Strongest Basic)
3.63
PSA
58.46 Å2
Refractivity
25.7 m3·mol-1
Polarizability
9.98 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Cơ Chế Tác Dụng : Imexon is a substance that is being studied in the treatment of some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma. It belongs to the family of drugs called cyanoaziridine derivatives. Also called Amplimexon. Imexon is a cyanoaziridine derivative. Imexon is a thiol-binding small molecule which induces mitochondrial oxidation, a loss of membrane potential and cytochrome C, leading to apoptosis. Imexon enters the cell and binds to glutathione and other sulfhydryl compounds, effectively preventing them from scavenging the toxic free radicals. So, particularly in the rapidly dividing cancer cell, free radical build-up in the presence of imexon leads to changes in mitochondrial membrane potential and ultimately to the mitochondria swelling and bursting. Mitochondrial proteins, in particular cytochrome c, are released into the cytoplasm and this activates caspase-mediated apoptosis resulting in cancer cell death. This sequence of events has been well characterized and published in several papers in leading cancer journals. Imexon is probably the only cancer drug under development at this time which exploits this mechanism of action. Imexon is an inhibitor of ribonucleotide reductase, a key enzyme in DNA synthesis that is also a target for gemcitabine. Imexon is also a cell cycle inhibitor and in the presence of the drug cells accumulate in S phase.
Chỉ Định : Investigated for use/treatment in melanoma, multiple myeloma, ovarian cancer, pancreatic cancer, and solid tumors.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Amplimexon
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05003
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=68791
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=11407098
ChemSpider
http://www.chemspider.com/Chemical-Structure.62031.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50073659
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