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  • BC-DXI-843
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BC-DXI-843

BC-DXI-843是一种有效的特异性AIMP2-DX2抑制剂,IC50为0.92μM,比作用于AIMP2(IC50>100μM)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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¥1237-5712
价格
990-4570
BC-DXI-843的二维码

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  • 货号: ajcx30240
  • CAS: 2421117-98-6
  • 别名:
  • 分子式: C28H26N4O4S2
  • 分子量: 546.66
  • 纯度: >98%
  • 溶解度: DMSO: 250 mg/mL (457.32 mM)
  • 储存: 4°C, protect from light
  • 库存: 现货

Background

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].


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]. Cell Proliferation Assay[1] Cell Line: A549 cancer cells and WI-26 normal cells


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


[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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