Tìm theo
Dactinomycin
Các tên gọi khác (10 ) :
  • 2-amino-N,N'-bis(hexadecahydro-2,5,9-trimethyl-6,13-bis(1-methylethyl)-1,4,7,11,14-pentaoxo-1H-pyrrolo(2,1-I)(1,4,7,10,13)oxatetra-azacyclohexadecin-10-yl)-4,6-dimethyl-3-oxo-3H-phenoxazine-1,9-dicarboxamide
  • ActD
  • Actinomycin C1
  • Actinomycin D
  • Actinomycin iv
  • Dactinomicina
  • Dactinomycin
  • Dactinomycine
  • Dactinomycinum
  • Meractinomycin
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 50-76-0
ATC: L01DA01
ĐG : Lundbeck Inc. , http://www.lundbeckinc.com
CTHH: C62H86N12O16
PTK: 1255.417
A compound composed of a two cyclic peptides attached to a phenoxazine that is derived from streptomyces parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C62H86N12O16
Phân tử khối
1255.417
Monoisotopic mass
1254.628474764
InChI
InChI=1S/C62H86N12O16/c1-27(2)42-59(84)73-23-17-19-36(73)57(82)69(13)25-38(75)71(15)48(29(5)6)61(86)88-33(11)44(55(80)65-42)67-53(78)35-22-21-31(9)51-46(35)64-47-40(41(63)50(77)32(10)52(47)90-51)54(79)68-45-34(12)89-62(87)49(30(7)8)72(16)39(76)26-70(14)58(83)37-20-18-24-74(37)60(85)43(28(3)4)66-56(45)81/h21-22,27-30,33-34,36-37,42-45,48-49H,17-20,23-26,63H2,1-16H3,(H,65,80)(H,66,81)(H,67,78)(H,68,79)/t33-,34-,36+,37+,42-,43-,44+,45+,48+,49+/m1/s1
InChI Key
InChIKey=RJURFGZVJUQBHK-IIXSONLDSA-N
IUPAC Name
1-N,9-N-bis[(6S,9R,10S,13R,18aS)-2,5,9-trimethyl-1,4,7,11,14-pentaoxo-6,13-bis(propan-2-yl)-hexadecahydro-1H-pyrrolo[2,1-i]1-oxa-4,7,10,13-tetraazacyclohexadecan-10-yl]-2-amino-4,6-dimethyl-3-oxo-3H-phenoxazine-1,9-dicarboxamide
Traditional IUPAC Name
actinomycin D
SMILES
[H][C@@]12CCCN1C(=O)[C@H](NC(=O)[C@@H](NC(=O)C1=C3N=C4C(OC3=C(C)C=C1)=C(C)C(=O)C(N)=C4C(=O)N[C@H]1[C@@H](C)OC(=O)[C@H](C(C)C)N(C)C(=O)CN(C)C(=O)[C@]3([H])CCCN3C(=O)[C@H](NC1=O)C(C)C)[C@@H](C)OC(=O)[C@H](C(C)C)N(C)C(=O)CN(C)C2=O)C(C)C
Độ tan chảy
241.5-243 °C
Độ hòa tan
Soluble at 10 °C
logP
1.6
logS
-4.8
pKa (strongest acidic)
10.52
pKa (Strongest Basic)
-0.13
PSA
355.54 Å2
Refractivity
326.17 m3·mol-1
Polarizability
129.2 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
16
H Bond Donor Count
5
Physiological Charge
0
Number of Rings
7
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Generally, the actinomycins exert an inhibitory effect on gram-positive and gram-negative bacteria and on some fungi. However, the toxic properties of the actinomycins (including dactinomycin) in relation to antibacterial activity are such as to preclude their use as antibiotics in the treatment of infectious diseases. Because the actinomycins are cytotoxic, they have an antineoplastic effect which has been demonstrated in experimental animals with various types of tumor implant. This cytotoxic action is the basis for their use in the treatment of certain types of cancer. Dactinomycin is believed to produce its cytotoxic effects by binding DNA and inhibiting RNA synthesis.
Cơ Chế Tác Dụng : A compound composed of a two cyclic peptides attached to a phenoxazine that is derived from streptomyces parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015) Good evidence exists that this drug bind strongly, but reversibly, to DNA, interfering with synthesis of RNA (prevention of RNA polymerase elongation) and, consequently, with protein synthesis.
Dược Động Học :
▧ Absorption :
poorly absorbed from gastrointestinal tract
▧ Protein binding :
5%
▧ Metabolism :
hepatic
▧ Half Life :
36 hours
Độc Tính : hepatoxicity
Chỉ Định : For the treatment of Wilms' tumor, childhood rhabdomyosarcoma, Ewing's sarcoma and metastatic, nonseminomatous testicular cancer as part of a combination chemotherapy and/or multi-modality treatment regimen
Tương Tác Thuốc :
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Cosmegen 0.5 mg vial
    Giá bán buôn : USD >684.36
    Đơn vị tính : vial
Nhà Sản Xuất
  • Công ty : Lundbeck
    Sản phẩm biệt dược : Cosmegen
  • Công ty : Lundbeck
    Sản phẩm biệt dược : Lyovac Cosmegen
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00970
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06770
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00214
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50023797
PharmGKB
http://www.pharmgkb.org/drug/PA151917012
Wikipedia
http://en.wikipedia.org/wiki/Dactinomycin
RxList
http://www.rxlist.com/cgi/generic2/dactinomycin.htm
Drugs.com
http://www.drugs.com/cdi/dactinomycin.html
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