Amsilarotene(Synonyms: TAC-101; Am 555S)

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Amsilarotene (Synonyms: TAC-101; Am 555S) 纯度: 99.70%

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。

Amsilarotene(Synonyms: TAC-101; Am 555S)

Amsilarotene Chemical Structure

CAS No. : 125973-56-0

规格 价格 是否有货 数量
5 mg ￥1800 In-stock
10 mg ￥2900 In-stock
25 mg ￥5800 In-stock
50 mg ￥9300 In-stock
100 mg ￥14500 In-stock
200 mg   询价  
500 mg   询价  

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Amsilarotene 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Transcription Factor Targeted Library
  • Anti-Liver Cancer Compound Library

生物活性

Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer[1][2][3].

IC50 & Target[1]

RARα

2.4 nM (Ki)

RARβ

400 nM (Ki)

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 G1 phase[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 G1 phase increased from 43% of untreated control cells to 86%

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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).

分子量

385.60

Formula

C20H27NO3Si2
CAS 号

125973-56-0
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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (259.34 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Sun SY, et al. Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells. Cancer Res. 1997 Nov 1;57(21):4931-9.

    [2]. Suzuki N, et al. A novel retinoid, 4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid (TAC-101), induces apoptosis of human ovarian carcinoma cells and shows potential as a new antitumor agent for clear cell adenocarcinoma. Gynecol Oncol. 2004 Sep;94(3):643-9.

    [3]. Fujimoto K, et al. Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44.

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