ASR-490,99.05%

产品编号:Bellancom-144899| CAS NO:2690312-67-3| 分子式:C34H41NO7| 分子量:575.69

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-144899
6500.00 杭州 北京(现货)
Bellancom-144899
10500.00 杭州 北京(现货)

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ASR-490

产品介绍 ASR-490 通过下调 Notch1 信号传导降低 HCT116 和 SW620 细胞的活力。ASR-490 克服 Notch1 的过表达并抑制 HCT/Notch1 转染子的生长。ASR-490 在异种移植小鼠中抑制对照 (pCMV/HCT116) 和 Notch1/HCT116 的肿瘤生长。
生物活性

ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

体外研究

ASR-490 (0-1.6 µM; 24 h, 48 h) reduces the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells). ASR-490 (750 nM in HCT116 cells and 1.2 µM in SW620 cells, 24 h) shows apoptotic cell death and upregulation of the proapoptotic markers Bax and cleaved PARP Expression; inhibits the capability of colorectal cancer cells. ASR-490 (HCT116 cells; 750 nM in 24 h, 600 nM in 48 h) overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: HCT116, SW620 cells
Concentration: 0-1.6 µM
Incubation Time: 24 h, 48 h
Result: Reduced the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells).

Apoptosis Analysis

Cell Line: HCT116, SW620 cells
Concentration: 750 nM in HCT116 cells and 1.2 µM in SW620 cells
Incubation Time: 24 h
Result: Showed apoptotic cell death and upregulation the proapoptotic markers Bax and cleaved PARP Expression, inhibited the capability of colorectal cancer cells.

Cell Proliferation Assay

Cell Line: HCT116 cells
Concentration: 750 nM in 24 h, 600 nM in 48 h
Incubation Time: 24 h, 48 h
Result: Overcome Notch1 overexpression and inhibited the growth of HCT/Notch1 transfectants.
体内研究
(In Vivo)

ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts).
Dosage: 5 mg/kg
Administration: i.p., thrice a week for 4 weeks
Result: Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.
体内研究

ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts).
Dosage: 5 mg/kg
Administration: i.p., thrice a week for 4 weeks
Result: Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.
体内研究

ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts).
Dosage: 5 mg/kg
Administration: i.p., thrice a week for 4 weeks
Result: Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.
性状Solid
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (43.43 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7370 mL 8.6852 mL 17.3705 mL
5 mM 0.3474 mL 1.7370 mL 3.4741 mL
10 mM 0.1737 mL 0.8685 mL 1.7370 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 (4.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.34 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 (4.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.34 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 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 (4.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.34 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 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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