Amsilarotene (TAC-101; Am 555S) 是一种具有口服活性的合成类视黄醇，对视黄酸受体 α (RAR-α) 具有选择性亲和力，对 RAR-α 和 RAR-β 的Ki值为 2.4 nM 和 400 nM。Amsilarotene 诱导人胃癌、肝细胞癌和卵巢癌细胞的凋亡 (apoptotic)。Amsilarotene 可用于癌症研究。
| 生物活性 | Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity forretinoic acid receptor α(RAR-α) binding withKiof 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces theapoptoticof human gastriccancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research ofcancer[1][2][3]. |
体外研究
(In Vitro) | Amsilarotene (0, 10, 25 μM; 24 hours) induces apoptosis of human epithelial ovarian carcinoma-derived cell lines in a concentration-dependent manner[2].
Amsilarotene (10, 20 μM; 0, 3, 6, and 9 days) inhibits the proliferation of BxPC-3 and MIAPaCa-2 cells[3].
Amsilarotene (10 μM; 48 hours) increases the proportion of sensitive BxPC-3 cells in the G1phase[3].
Amsilarotene (10 μM; 0, 3, 6, 24, 48, 72 hours) inhibits the retinoblastoma-gene product (RB) phosphorylation in BxPC-3 cells between 24 and 72 hours[3].
Apoptosis Analysis[2] | Cell Line: | RMG-I, RMG-II, RTSG, RMUG-S, RMUG-L, and KF cells | | Concentration: | 0, 10, 25 μM | | Incubation Time: | 24 hours | | Result: | Induced apoptosis in a concentration-dependent manner in all of the cell lines, except KF cells. |
Cell Proliferation Assay[3] | Cell Line: | BxPC-3, MIAPaCa-2, AsPC-1 cells | | Concentration: | 10 and 20 μM | | Incubation Time: | 0, 3, 6, and 9 days. | | Result: | Inhibited the proliferation of BxPC-3 and MIAPaCa-2 cells, but not the proliferation of AsPC-1 cells. |
Cell Cycle Analysis[3] | Cell Line: | Sensitive BxPC-3 cells | | Concentration: | 10 μM | | Incubation Time: | 48 hours | | Result: | The proportion of cells in the G1phase increased from 43% of untreated control cells to 86% |
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体内研究
(In Vivo) | Amsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice[2].
| Animal Model: | 6-week-old female BALB/c nu/nu mice with subcutaneous RMG-II tumors[2] | | Dosage: | 8 mg/kg/day | | Administration: | Orally for 30 days | | Result: | The maximal tumor growth-inhibiting effect was seen on day 31 of administration, when there was a 45% reduction of relative tumor volume (RTV). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(259.34 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5934 mL | 12.9668 mL | 25.9336 mL | | 5 mM | 0.5187 mL | 2.5934 mL | 5.1867 mL | | 10 mM | 0.2593 mL | 1.2967 mL | 2.5934 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.48 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (6.48 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.48 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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