BC-DXI-843

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BC-DXI-843  纯度: 98.73%

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。

BC-DXI-843

BC-DXI-843 Chemical Structure

CAS No. : 2421117-98-6

规格 价格 是否有货 数量
5 mg ￥1150 In-stock
10 mg ￥1900 In-stock
25 mg ￥3500 In-stock
50 mg ￥5300 In-stock
100 mg   询价  
200 mg   询价  

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BC-DXI-843 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Targeted Diversity Library

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[1].

IC50 & Target

IC50: 0.92 μM (AIMP2-DX2), IC50: >100 μM (AIMP2)[1]
体外研究
(In Vitro)

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[1].

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.

Cell Proliferation Assay[1]

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
(In Vivo)

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)[1].

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 Model: 7-week-old female BALB/cSLC-nu/nu mice bearing H460 cells xenograft[1]
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.

分子量

546.66

Formula

C28H26N4O4S2
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。

    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

*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]. Aneesh Sivaraman, et al. Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy. J Med Chem. 2020 May 28;63(10):5139-5158.

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