Tìm theo
Tamibarotene
Các tên gọi khác (5 ) :
  • Am 80
  • Amnoid
  • retinobenzoic acid
  • Tamibaro
  • Tamibarotene
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 94497-51-5
CTHH: C22H25NO3
PTK: 351.4388
Tamibarotene is a novel synthetic retinoid for acute promyelocytic leukaemia (APL). Tamibarotene is currently approved in Japan for treatment of recurrent APL, and is undergoing clinical trials in the United States.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H25NO3
Phân tử khối
351.4388
Monoisotopic mass
351.183443671
InChI
InChI=1S/C22H25NO3/c1-21(2)11-12-22(3,4)18-13-16(9-10-17(18)21)23-19(24)14-5-7-15(8-6-14)20(25)26/h5-10,13H,11-12H2,1-4H3,(H,23,24)(H,25,26)
InChI Key
InChIKey=MUTNCGKQJGXKEM-UHFFFAOYSA-N
IUPAC Name
4-[(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbamoyl]benzoic acid
Traditional IUPAC Name
tamibarotene
SMILES
CC1(C)CCC(C)(C)C2=C1C=CC(NC(=O)C1=CC=C(C=C1)C(O)=O)=C2
Độ hòa tan
5.75e-04 g/l
logP
5.35
logS
-5.8
pKa (strongest acidic)
3.69
pKa (Strongest Basic)
-4
PSA
66.4 Å2
Refractivity
104.38 m3·mol-1
Polarizability
39.16 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Ghose Filter
true
Dược Lực Học : Tamibarotene is a new synthetic retinoid drug recently approved for relapsed or refractory acute promyelocytic leukemia (APL) in Japan. It is a specific agonist for retinoic acid receptor alpha/beta. Compared to all-trans retinoic acid (ATRA), a natural retinoid indicated for a first-line treatment of APL, tamibarotene is chemically more stable and several times more potent as an inducer of differentiation in promyelocytic leukemia cells. In contrast to ATRA, whose plasma concentration declines considerably during daily administration, tamibarotene sustains plasma level probably due to a lower affinity for cellular retinoic acid binding protein. Furthermore, adverse side effects were milder than those of ATRA in clinical trials.
Cơ Chế Tác Dụng : Tamibarotene is a novel synthetic retinoid for acute promyelocytic leukaemia (APL). Tamibarotene is currently approved in Japan for treatment of recurrent APL, and is undergoing clinical trials in the United States. Tamibarotene is a specific agonist for retinoic acid receptor alpha/beta with possible binding to retinoid X receptors (RXR).
Dược Động Học :

▧ Protein binding :
Over 99%, predominantly to serum albumin.
Chỉ Định : Investigated for use/treatment in leukemia (unspecified).
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Amnoid
  • Công ty :
    Sản phẩm biệt dược : Tamibaro
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04942
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=108143
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509039
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C12864
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01418
ChemSpider
http://www.chemspider.com/Chemical-Structure.97231.html
PharmGKB
http://www.pharmgkb.org/drug/PA164743464
Wikipedia
http://en.wikipedia.org/wiki/Tamibarotene
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