他米巴罗汀 T6694

Product Introduction
Bioactivity


英文名: Tamibarotene

描述: Tamibarotene (Amnolake) 是一种具有口服活性的合成维甲酸，旨在克服全反式维甲酸耐药性，具有潜在的抗肿瘤活性。它也是视黄酸受体α/β 的激动剂，比RARγ的选择性高。

细胞实验: 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.

体外活性: Tamibarotene治疗明显降低小鼠的脑中不溶性Aβ水平,特别是Aβ（42）,而Tamibarotene对可溶性Aβ水平没有明显影响.

体内活性: Tamibarotene诱导的HL-60细胞粘附到内皮细胞比全反式维甲酸低38％,Tamibarotene诱导NB4细胞粘附到内皮细胞的能力和ATRA相当,其在HL-60中两相诱导CD38基因转录细胞,通过含有内含子1的DR-RARE的早期相诱导和通过缺乏5'侧翼区的RARE的延迟相诱导。Tamibarotene仅诱导HL-60细胞的早期诱导,导致比ATRA低的CD38诱导。Tamibarotene对外周血单核细胞的生长抑制可以忽略不计,但对HTLV-I感染T细胞系和ATL细胞的标记的生长抑制很强。Tamibarotene使HTLV-I感染T细胞系细胞停留在细胞周期的G1期,并诱导细胞凋亡。Tamibarotene也抑制IkappaBalpha的磷酸化和NF-κB-DNA结合,并减少参与G1/S期细胞周期的过渡和凋亡蛋白表达。Tamibarotene也抑制JunD的表达,从而抑制AP-1的DNA结合。Tamibarotene略微抑制了骨髓瘤细胞和HUVEC的生长,并显着抑制由VEGF刺激的HUVEC的生长。Tamibarotene显示对骨髓基质细胞（BMSC）的生长抑制很小,但通过共培养骨髓瘤细胞显着抑制HUVEC的迁移。Tamibarotene抑制VEGF诱导的VEGF受体的磷酸化。Tamibarotene明显抑制小鼠角膜中VEGF诱导的体外管样结构的形成和新生血管的形成。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (170.73 mM)
1.1eq. NaOH : 35.1 mg/mL (100 mM)


关键字: Autophagy | Apoptosis | NSC-608000 | Am-80 | Retinoid X receptors | NSC608000 | Inhibitor | Am80 | RAR/RXR | Tamibarotene | Retinoic acid receptors | inhibit

相关产品: Apoptosis inducer 11 | 2-Deoxy-D-glucose | Clitocine | Xanthohumol | IITZ-01 | Ginsenoside Rk1 | ROC-325 | Arctigenin | R406 | Didymin

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Neuronal Differentiation Compound Library | Anti-Metabolism Disease Compound Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Metabolism Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途