Tìm theo
AZD2171
Thuốc Gốc
Small Molecule
CTHH: C25H27FN4O3
PTK: 450.5053
The novel indole-ether quinazoline AZD2171 is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro. It is being developed clinically as a once-daily oral therapy for the treatment of cancer.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H27FN4O3
Phân tử khối
450.5053
Monoisotopic mass
450.206718955
InChI
InChI=1S/C25H27FN4O3/c1-16-12-17-19(29-16)6-7-21(24(17)26)33-25-18-13-22(31-2)23(14-20(18)27-15-28-25)32-11-5-10-30-8-3-4-9-30/h6-7,12-15,29H,3-5,8-11H2,1-2H3
InChI Key
InChIKey=XXJWYDDUDKYVKI-UHFFFAOYSA-N
IUPAC Name
4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline
Traditional IUPAC Name
cediranib
SMILES
COC1=CC2=C(C=C1OCCCN1CCCC1)N=CN=C2OC1=C(F)C2=C(NC(C)=C2)C=C1
Độ hòa tan
1.55e-02 g/l
logP
4.13
logS
-4.5
pKa (strongest acidic)
16.59
pKa (Strongest Basic)
9.14
PSA
72.5 Å2
Refractivity
125.16 m3·mol-1
Polarizability
48.77 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : AZD2171 is a once-daily, orally available, highly potent and selective VEGF signalling inhibitor that inhibits all three VEGF receptors. The preclinical profile of AZD2171 indicates that it has the potential to be the 'best in class' VEGF signalling inhibitor. Phase I data indicate that AZD2171 is generally well tolerated, with the most common dose related adverse events being diarrhoea, hoarseness, headache and hypertension.
Cơ Chế Tác Dụng : The novel indole-ether quinazoline AZD2171 is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro. It is being developed clinically as a once-daily oral therapy for the treatment of cancer. AZD2171 inhibits vacular endothelial growth factor (VEGF) receptor tyrosine kinase (RTK). By forming a blockade at the VEGF receptors, AZD2171 limits the growth of new blood vessels, which are essential to supporting tumor growth. Thus, lacking sufficient blood supply, tumor cells become starved for nutrients, slowing or halting growth and potentially improving the efficacy of other treatments. Preclinical evidence indicated that the drug had a high affinity at these sites, and was well tolerated and efficacious in animal studies.
Dược Động Học :
▧ Absorption :
Available following oral administration.
▧ Half Life :
12 to 35 hours
Chỉ Định : For the treatment of liver cancer, advanced non-small cell lung cancer (NSCLC), advanced colorectal cancer (CRC) and other solid tumors.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Recentin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04849
ChemSpider
http://www.chemspider.com/Chemical-Structure.8109103.html
Wikipedia
http://en.wikipedia.org/wiki/AZD2171
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