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维生素D相关/核受体
代谢酶 PPAR Signaling Pathway
/ RAR/RXR / Tamibarotene

他米巴罗汀 /Tamibarotene {[allProObj[0].p_purity_real_show]}

货号：A197861 同义名： Am 80;Amnolake

Tamibarotene是一种视黄酸受体 α（RARα）激动剂，ED50 为 0.79 nM，可诱导 HL-60 细胞的分化和凋亡，适用于急性白血病研究。

Tamibarotene 化学结构 CAS号：94497-51-5
Tamibarotene 化学结构
CAS号：94497-51-5
Tamibarotene 3D分子结构
CAS号：94497-51-5
Tamibarotene 化学结构 CAS号：94497-51-5
Tamibarotene 3D分子结构 CAS号：94497-51-5
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Tamibarotene 纯度/质量文件 产品仅供科研

货号：A197861 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

• ACS Appl. Nano Mater., 2025. Ambeed. [ A188026 ]
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• JJC, 2025, 20(Special Issue)): 27-39. Ambeed. [ A713856 ]
• bioRxiv, 2025. Ambeed. [ A538667 , A714873 , A126729 , A126049 , A446054 ]
• Nature Communications, 2025, 16, 1871. Ambeed. [ A508148 ]
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Tamibarotene 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].

Tamibarotene 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
Jurkat cells Proliferation assay Antiproliferative activity against human Jurkat cells, IC50=17.3 μM 19443225

Tamibarotene 动物研究

Dose Mice: 2.5 mg/kg[3] (p.o.); 15 mg/kg[4] (i.p.) Rat: 2 mg/kg - 10 mg/kg[5] (p.o.)
Administration p.o., i.p.

Tamibarotene 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 <<

Tamibarotene 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.

Tamibarotene 实验方案

计算器
存储液制备 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

Tamibarotene 技术信息

CAS号94497-51-5
分子式C22H25NO3
分子量 351.439
别名 Am 80;Amnolake;SY-1425;Retinobenzoic acid, Amnoid, AMNOLAKE, Am80, Am 80, Am-80;Retinobenzoic Acid;NSC 608000
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
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

Tags: Tamibarotene | Am 80;Amnolake;SY-1425;Retinobenzoic acid, Amnoid, AMNOLAKE, Am80, Am 80, Am-80;Retinobenzoic Acid;NSC 608000 | RAR/RXR | AmBeed-信号通路专用抑制剂 | Tamibarotene 纯度/质量文件 | Tamibarotene 生物活性 | Tamibarotene 细胞研究 | Tamibarotene 动物研究 | Tamibarotene 临床数据 | Tamibarotene 参考文献 | Tamibarotene 实验方案 | Tamibarotene 技术信息

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