Tamibarotene

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Chemical Structure| 94497-51-5 同义名 : Am 80;Amnolake;SY-1425;Retinobenzoic acid, Amnoid, AMNOLAKE, Am80, Am 80, Am-80;Retinobenzoic Acid;NSC 608000
CAS号 : 94497-51-5
货号 : A197861
分子式 : C22H25NO3
纯度 : 98%
分子量 : 351.439
MDL号 : MFCD00866188
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(71.14 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 56 mg/mL suspension

生物活性
描述 Retinoid acid (RA) is a metabolite of retinol that plays an important role in cell growth and differentiation. The retinoic acid receptors (RARs) and retinoid X receptors (RXRs) are two classes of nuclear receptors mediating the regulation of RA and its derivatives on gene expression. Tamibarotene is a RAR agonist selective for RARa with an Kd value of 62 nM and an AC50 value of 1.46 nM compared to RARb (Kd = 280 nM, AC50 = 6.87 nM) and RARg (Kd = 816 nM, AC50 = 148.66 nM)[3]. Incubation of HL-60 cells with tamibarotene (100 nM – 10 μM) for 9 days significantly decreased the total cell number and increased the number of dead cells at a time-dependent manner. The percentage of growth inhibition induced by 100 nM tamibarotene after 9-day incubation was 32.0, 23.7, 27.9, and 59.2% in HL60R, K562, Kasumi-1, and Meg01 cells, respectively. Tamibarotene at 10, 20, and 40 μM also induced the secretion of TGF-b2 in K562, MOLT3, Raji, and U937 cell lines with an incubation period of 3 days. Moreover, 3-day treatment of tamibarotene from 10 – 40 μM in Raji cells increased the expression ratio of phosphorylated Smad-2 relative to Smad-2 at a dose-dependent manner[4]. In C57BL/6J mice, oral administration of tamibarotene (5 mg/kg, once per day) for 4 days prevented intracerebral hemorrhage-induced neuron loss compared to vehicle-treated group. The same treatment also decreased the number of activated microglia/macrophages and the expression of HO-1 associated with intracerebral hemorrhage[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
COS-1 cells Function assay Transcriptional activation in COS-1 cells expressing Retinoic Acid Receptor alpha (RAR alpha) 10669568
HL60 cells Proliferation assay Antiproliferative activity against human HL60 cells, IC50=6 μM 19443225
HL60 cells Proliferation assay 48 h Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50=8.94 μM 22014829
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02807558 Acute Myeloid Leukemia ... 展开 >> Myelodysplastic Syndrome 收起 << Phase 2 Recruiting December 2021 United States, Iowa ... 展开 >> Recruiting Iowa City, Iowa, United States United States, Massachusetts Recruiting Boston, Massachusetts, United States United States, Michigan Recruiting Ann Arbor, Michigan, United States United States, New York Recruiting New York, New York, United States Recruiting Rochester, New York, United States United States, North Carolina Recruiting Durham, North Carolina, United States United States, Ohio Recruiting Cleveland, Ohio, United States United States, Oregon Recruiting Portland, Oregon, United States United States, Pennsylvania Recruiting Pittsburgh, Pennsylvania, United States United States, Tennessee Recruiting Nashville, Tennessee, United States United States, Texas Recruiting Houston, Texas, United States France Centre Hospitalier Universitaire Nancy Recruiting Vandoeuvre les nancy, France, 54511 Institut Gustave Roussy Recruiting Villejuif, France, 94805 收起 <<
NCT00417391 Crohn's Disease Phase 2 Completed - Japan ... 展开 >> Toyohashi, Aichi, Japan Sakura, Chiba, Japan Sapporo, Hokkaido, Japan Nishinomiya, Hyogo, Japan Fujisawa, Kanagawa, Japan Nakagami, Okinawa, Japan Otsu, Shiga, Japan Shinjuku, Tokyo, Japan 收起 <<
NCT01226147 Lupus Nephritis Phase 2 Unknown February 2013 Japan ... 展开 >> Kinki University Hospital Recruiting Osaka, Japan, 5898511 Contact: Masanori Funauchi, M.D.       mn-funa@med.kindai.ac.jp    Principal Investigator: Masanori Funauchi, M.D. 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.28mL

14.23mL

2.85mL

1.42mL

28.45mL

5.69mL

2.85mL
参考文献

[1]Uruno A, Noguchi N, et al. All-trans retinoic acid and a novel synthetic retinoid tamibarotene (Am80) differentially regulate CD38 expression in human leukemia HL-60 cells: possible involvement of protein kinase C-delta. J Leukoc Biol. 2011 Aug;90(2):235-47.

[2]Sanda T, Kuwano T, et al. Antimyeloma effects of a novel synthetic retinoid Am80 (Tamibarotene) through inhibition of angiogenesis. Leukemia. 2005 Jun;19(6):901-9.

[3]Bernard BA, Bernardon JM, Delescluse C, Martin B, Lenoir MC, Maignan J, Charpentier B, Pilgrim WR, Reichert U, Shroot B. Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma. Biochem Biophys Res Commun. 1992 Jul 31;186(2):977-83.

[4]Jimi S, Mashima K, Matsumoto T, Hara S, Suzumiya J, Tamura K. RARalpha is a regulatory factor for Am-80-induced cell growth inhibition of hematologic malignant cells. Int J Oncol. 2007 Aug;31(2):397-404.

[5]Matsushita H, Hijioka M, Hisatsune A, Isohama Y, Shudo K, Katsuki H. A retinoic acid receptor agonist Am80 rescues neurons, attenuates inflammatory reactions, and improves behavioral recovery after intracerebral hemorrhage in mice. J Cereb Blood Flow Metab. 2011 Jan;31(1):222-34.