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BC-DXI-843
目录号 : KM5142 CAS No. : 2421117-98-6 纯度 : 98%

BC-DXI-843 是一种有效的特异性 AIMP2-DX2 抑制剂,IC50 为 0.92 μM,比作用于 AIMP2 (IC50 >100 μM) 选择性高 100 倍以上。BC-DXI-843 有潜力用于 AIMP2-DX2 肺癌的研究。

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5mg
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10mg
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25mg
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50mg
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100mg 询价 In-stock
200mg 询价 In-stock

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生物活性

BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC50 of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer.

体外研究

BC-DXI-843 (0.0316-31.6 μM; 72 hours) suppresses cancer cell proliferation in a DX2-dependent manner. The EC50 in A549 cells is 1.20 μM, which is similar to the IC50 for inhibition of DX2. However, no inhibition of WI-26 cells is observed, suggesting that BC-DXI-843 specifically reduces the viability of cancer cells.

Cell Proliferation Assay

Cell Line: A549 cancer cells and WI-26 normal cells
Concentration: 0.0316, 0.1, 0.316, 1, 3.16, 10, 31.6 μM
Incubation Time: 72 hours
Result: The EC50 in A549 cells was 1.20 μM. No inhibition of WI-26 cells was observed.
体内研究

BC-DXI-843 (50 mg/kg; intraperitoneally administered; every other day for 15 days) demonstrates in vivo efficacy in a tumor xenograft mouse model (H460 cells).

Animal Model: 7-week-old female BALB/cSLC-nu/nu mice bearing H460 cells xenograft
Dosage: 50 mg/kg
Administration: Intraperitoneally administered; every other day for 15 days
Result: The embedded tumor volume gradually declined after BC-DXI-843administration, but no changes in body weight were observed. The weight of the excised tumors after sacrifice had decreased in mice.
分子式
C28H26N4O4S2
分子量
546.66
CAS号
2421117-98-6
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (457.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8293 mL 9.1465 mL 18.2929 mL
5 mM 0.3659 mL 1.8293 mL 3.6586 mL
10 mM 0.1829 mL 0.9146 mL 1.8293 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 (protect from light)。-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: ≥ 2.08 mg/mL (3.80 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.80 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

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