Tìm theo
Vindesine
Các tên gọi khác (3) :
  • 3-(Aminocarbonyl)-O(4)-deacetyl-3-de(methoxycarbonyl)vincaleukoblastine
  • 3-Carbamoyl-4-deacetyl-3-de(methoxycarbonyl)vincaleukoblastine
  • Desacetylvinblastine amide
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 53643-48-4
ATC: L01CA03
CTHH: C43H55N5O7
PTK: 753.9261
Vinblastine derivative with antineoplastic activity against cancer. Major side effects are myelosuppression and neurotoxicity. Vindesine is used extensively in chemotherapy protocols (antineoplastic combined chemotherapy protocols). [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C43H55N5O7
Phân tử khối
753.9261
Monoisotopic mass
753.410149139
InChI
InChI=1S/C43H55N5O7/c1-6-39(52)21-25-22-42(38(51)55-5,33-27(13-17-47(23-25)24-39)26-11-8-9-12-30(26)45-33)29-19-28-31(20-32(29)54-4)46(3)35-41(28)15-18-48-16-10-14-40(7-2,34(41)48)36(49)43(35,53)37(44)50/h8-12,14,19-20,25,34-36,45,49,52-53H,6-7,13,15-18,21-24H2,1-5H3,(H2,44,50)/t25-,34+,35-,36-,39+,40-,41-,42+,43+/m1/s1
InChI Key
InChIKey=HHJUWIANJFBDHT-KOTLKJBCSA-N
IUPAC Name
methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-carbamoyl-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.0^{1,9}.0^{2,7}.0^{16,19}]nonadeca-2(7),3,5,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.0^{4,12}.0^{5,10}]nonadeca-4(12),5,7,9-tetraene-13-carboxylate
Traditional IUPAC Name
vindesine
SMILES
[H][C@@]12N3CC[C@@]11C4=CC(=C(OC)C=C4N(C)[C@@]1([H])[C@](O)([C@H](O)[C@]2(CC)C=CC3)C(N)=O)[C@]1(C[C@]2([H])CN(C[C@](O)(CC)C2)CCC2=C1NC1=CC=CC=C21)C(=O)OC
Độ tan chảy
230-232 °C
Độ hòa tan
7.00e-02 g/l
logP
2.9
logS
-4
pKa (strongest acidic)
11.34
pKa (Strongest Basic)
8.68
PSA
164.82 Å2
Refractivity
210.32 m3·mol-1
Polarizability
82.58 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
9
H Bond Donor Count
5
Physiological Charge
2
Number of Rings
9
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Vindesine is indicated for the treatment of acute lymphocytic leukemia of childhood that is resistant to vincristine and non-oat cell lung cancer.Vindesine causes the arrest of cells in metaphase mitosis. It is three times more potent than vincristine and nearly 10 times more potent than vinblastine in causing mitotic arrest in in vitro studies at doses designed to arrest from 10 to 15% of the cells in mitosis. Vindesine and vincristine are approximately equipotent at dose levels that arrest 40 to 50% of the cells in mitosis. Unlike vinblastine, vindesine produces very few postmetaphase cells. Vindesine has demonstrated activity in patients who have relapsed while receiving multiple-agent treatment that included vincristine.
Cơ Chế Tác Dụng : Vinblastine derivative with antineoplastic activity against cancer. Major side effects are myelosuppression and neurotoxicity. Vindesine is used extensively in chemotherapy protocols (antineoplastic combined chemotherapy protocols). [PubChem] Vindesine acts by causing the arrest of cells in metaphase mitosis through its inhibition tubulin mitotic funcitoning. The drug is cell-cycle specific for the S phase.
Dược Động Học :

▧ Protein binding :
65-75%
▧ Metabolism :
Hepatic
▧ Half Life :
24 hours.
Chỉ Định : For the treatment of acute leukaemia, malignant lymphoma, Hodgkin's disease, acute erythraemia and acute panmyelosis
Tương Tác Thuốc :
  • Mitomycin Potentially severe lung toxicity
  • Quinupristin This combination presents an increased risk of toxicity
Liều Lượng & Cách Dùng : Solution - Intravenous
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Eldesine
  • Công ty :
    Sản phẩm biệt dược : Eldisine
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00309
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=40839
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504548
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01769
ChemSpider
http://www.chemspider.com/Chemical-Structure.37302.html
PharmGKB
http://www.pharmgkb.org/drug/PA10232
Wikipedia
http://en.wikipedia.org/wiki/Vindesine
RxList
http://www.rxlist.com/cgi/generic2/vinor_cp.htm
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