3α-Aminocholestane(Synonyms: 3α-氨基胆甾烷)

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3α-Aminocholestane (Synonyms: 3α-氨基胆甾烷) 纯度: ≥98.0%

3α-Aminocholestane 是含有选择性 SH2 结构域的肌醇-5′-磷酸酶 1 (SHIP1) 的抑制剂,其 IC50 值约为 2.5 μM。

3α-Aminocholestane(Synonyms: 3α-氨基胆甾烷)

3α-Aminocholestane Chemical Structure

CAS No. : 2206-20-4

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10 mM * 1 mL in Ethanol ¥938 In-stock
5 mg ¥1100 In-stock
10 mg ¥1800 In-stock
25 mg ¥3600 In-stock
50 mg ¥5600 In-stock
100 mg ¥8900 In-stock
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3α-Aminocholestane 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Phosphatase Inhibitor Library

生物活性

3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.

IC50 & Target

IC50: 2.5 μM (SHIP1)[1]

体外研究
(In Vitro)

OPM2 cell viability is effectively reduced by 3α-Aminocholestane (3AC) treatment. RPMI8226 and U266 cells show significantly less sensitivity to 3α-Aminocholestane treatment when compare with OPM2 cells, although viability is decreased significantly at concentrations of ≥12.5 μM. Treatment with 3α-Aminocholestane for 36 h severely reduces the percentage of cells in the S phase, which is accompanied by an increase of cells in the G2/M phase. In contrast, in the less proliferative RPMI8226 and U266 cells, cell cycle progression is blocked in the G0/G1 phase upon 3α-Aminocholestane treatment, in conjunction with a reduced percentage of cells undergoing the S phase[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

It is found that 3α-Aminocholestane (3AC) results in reduced multiple myeloma (MM) growth in vivo, as determined by quantitation of free human Igλ light chain in the plasma after OPM2 challenge. In addition, reduced numbers of circulating OPM2 cells, as determined by human HLA-ABC staining, is observed in peripheral blood from 3α-Aminocholestane-treated mice compare with vehicle controls. Most importantly, 3α-Aminocholestane treatment results in significantly enhanced survival of mice after tumor challenge. In 3α-Aminocholestane-treated mice that resist treatment, it is found that MM tumors exhibit an upregulation of SHIP2, reminiscent of in vitro treatment of OPM2 cells and suggesting that SHIP1 inhibition may select for tumor cells with increased SHIP2 expression[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

387.68

Formula

C27H49N

CAS 号

2206-20-4

中文名称

3α-氨基胆甾烷;3alpha-氨基胆甾烷

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: 

Ethanol : 50 mg/mL (128.97 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5794 mL 12.8972 mL 25.7945 mL
5 mM 0.5159 mL 2.5794 mL 5.1589 mL
10 mM 0.2579 mL 1.2897 mL 2.5794 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% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.25 mg/mL (8.38 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (8.38 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 EtOH 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% EtOH    90% corn oil

    Solubility: ≥ 3.25 mg/mL (8.38 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (8.38 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 32.5 mg/mL 的澄清 EtOH 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Chen Z, et al. Signalling thresholds and negative B-cell selection in acute lymphoblastic leukaemia. Nature. 2015 May 21;521(7552):357-61.

    [2]. Gwenny M Fuhler, et al. Therapeutic Potential of SH2 Domain-Containing Inositol-5′-Phosphatase 1 (SHIP1) and SHIP2 Inhibition in Cancer. Mol Med. 2012 Feb 10;18:65-75.

Cell Assay
[2]

Cells are treated in triplicate or more with increasing concentrations of compounds (including 3α-Aminocholestane). Cell viability is determined with a Cell Counting Kit according to the manufacturer’s instructions. The odds density (OD) of compound (including 3α-Aminocholestane )-treated cells is divided by the OD of their vehicle control, and the viability is expressed as a percentage of untreated cells. Results are expressed as mean±standard error of the mean (SEM) of three individual experiments. For phosphatidyl inositol phosphates (PIP) add-back experiments, MCF-7 cells are treated for 2 h with 10 μM SHIP inhibitors (including 3α-Aminocholestane ), after which cells are washed and fresh medium is added. Cells are subsequently cultured in the absence (0 μM) or presence (10 or 20 μM) of either PtdIns(3,4)P2-diC16 (P-3416) or PtdIns(3,5)P2-diC16 (P-3516) for 36 h, after which cell viability is determined by the Cell Counting Kit[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

NOD/SCID/γcIL2R (NSG) mice are injected intraperitoneally with 1×107 OPM2 cells and 6 h later receive an initial injection of 3α-Aminocholestane (3AC) or vehicle. 3α-Aminocholestane is suspended in a 0.3% Klucel/H2O solution at 11.46 mM and administered by intraperitoneal injection of 100 μL solution. Vehicle-treated mice receive 100 μL injection of 0.3% Klucel/H2O solution. The mice are then treated with 3α-Aminocholestane or vehicle daily for the next 6 d and then twice per week in the remaining 15 wks of the survival study[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Chen Z, et al. Signalling thresholds and negative B-cell selection in acute lymphoblastic leukaemia. Nature. 2015 May 21;521(7552):357-61.

    [2]. Gwenny M Fuhler, et al. Therapeutic Potential of SH2 Domain-Containing Inositol-5′-Phosphatase 1 (SHIP1) and SHIP2 Inhibition in Cancer. Mol Med. 2012 Feb 10;18:65-75.

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