您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Tamibarotene
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Tamibarotene
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tamibarotene图片
CAS NO:94497-51-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)351.44
FormulaC22H25NO3
CAS No.94497-51-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 70 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 70 mg/mL (199.2 mM)
SMILES CodeO=C(O)C1=CC=C(C(NC2=CC=C3C(C)(C)CCC(C)(C)C3=C2)=O)C=C1
SynonymsSY-1425; Am80, SY 1425; Am 80, SY1425; Retinobenzoic acid, Amnoid, AMNOLAKE, Am-80;
实验参考方法
In Vitro

In vitro activity: Tamibarotene slightly inhibits the growth of both myeloma cells and HUVECs, and remarkably inhibits the growth of HUVECs stimulated by VEGF. Tamibarotene shows little growth inhibition of bone marrow stromal cells (BMSCs), but it markedly inhibits migration of HUVECs by cocultured myeloma cells. Tamibarotene inhibits VEGF-induced phosphorylation of VEGF receptor. Tamibarotene significantly inhibits VEGF-induced formation of tube-like structures in vitro and neovascularization in mouse corneas. Tamibarotene-induced HL-60 cell adhesion to ECs is 38% lower than All-trans retinoic acid (ATRA), and NB4 cell adhesion to ECs by tamibarotene is equivalent to ATRA, which induces CD38 gene transcription biphasically in HL-60 cells, the early-phase induction via DR-RARE containing intron 1, and the delayed-phase induction via RARE lacking the 5'-flanking region. Tamibarotene induces only the early-phase induction in HL-60 cells, resulting in its lower CD38 induction than ATRA. Tamibarotene has negligible growth inhibition of peripheral blood mononuclear cells but marked growth inhibition of both HTLV-I-infected T-cell lines and ATL cells. Tamibarotene arrests cells in the G1 phase of the cell cycle and induces apoptosis in HTLV-I-infected T-cell lines. Tamibarotene inhibits also the phosphorylation of IkappaBalpha and NF-kappaB-DNA binding, in conjunction with reduction of expression of proteins involved in the G1/S cell cycle transition and apoptosis. Tamibarotene also inhibits the expression of JunD, resulting in suppression of AP-1-DNA binding.


Kinase Assay: Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist with high selectivity over RARγ.


Cell Assay: The CellTiter Aqueous Non-Radioactive Cell Proliferation Assay Kit is used to assess cell growth. Briefly, 10,000 cells per well are seeded in a 96-well plate and cultured in RPMI containing 2% charcoal-stripped FBS and indicated retinoid concentrations for 72 hours. At the end of the treatment period, the MTS reagent is added, cells are incubated an additional 2-4 hours, and absorbance is measured at 490 nanometers.

In VivoTamibarotene treatment reduces significantly the insoluble Abeta levels in brain of mice, in particular Abeta(42), while it gives no apparent effects on the soluble Abeta levels.
Animal modelMice:For the infection, mice are given sulfamethoxazole and trimethoprim in an oral suspension at 10 mL of deionized water ad libitum for 10 days to reduce the native flora and to support colonization of P. gingivalis W83. Four days after the antibiotic therapy finishes, periodontal infection is established through oral inoculation using 1010 colony-forming units of P. gingivalis suspended in 100 μL 4% carboxymethyl cellulose (CMC) for 7 days. The mice are euthanized 4 weeks after the first oral inoculation. Tamibarotene (2.5 mg/kg) is suspended in a 0.5% carboxymethyl cellulose solution. The drug is orally gavaged into the esophagus daily in a volume of 0.1 mL/10 g body weight. Tamibarotene is administered 1 h before the induction of periodontitis and then given daily per the protocol until day 28. Control mice with periodontal disease receive the same volume of 0.5% carboxymethyl cellulose solution. The body weight of each mouse is measured every 3 days.
Formulation & Dosage2.5 mg/kg; oral
ReferencesLeukemia. 2005 Jun;19(6):901-9; J Leukoc Biol. 2011 Aug;90(2):235-47; Biol Pharm Bull. 2009 Jul;32(7):1307-9.