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CAS No.: 2421117-98-6

BC-DXI-843 Catalog No. CSN26134

BC-DXI-843 is an AIMP2-DX2 inhibitor with IC50 value of 0.92μM. It demonstrated in vivo efficacy in a tumor xenograft mouse model (H460 cells) at a dosage of 50 mg/kg.

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400-920-2911

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技术信息

生物活性

描述AIMP2-DX2, a splicing variant of AIMP2, is up-regulated in lung cancer, possesses oncogenic activity, and results in tumorigenesis. BC-DXI-843 is a potent and selective AIMP2-DX2 inhibitor with an IC₅₀ value of 0.92 μM which is more than 100-fold selectivity over AIMP2 (IC₅₀ >100 μM) in a luciferase assay. In H460 cells, BC-DXI-843 exhibited dose-dependent inhibition of DX2 protein levels, and it efficiently induced degradation of DX2 at a very low concentration of 1.20 μM. Moreover, BC-DXI-843 demonstrated in vivo efficacy in a tumor xenograft mouse model (H460 cells) at a dosage of 50 mg/kg, suggesting it as a promising lead for development of novel therapeutics targeting AIMP2-DX2 in lung cancer^[1].
作用机制BC-DXI-843 was positioned very close to L80, T82, F116, T117, and K129 and it forms two hydrogen bonds with the hydrophobic pocket via T82 and D52^[1].
参考文献

[1] Sivaraman A, Kim DG, Bhattarai D, 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;63(10):5139-5158

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8293 mL
- 9.1464 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

技术信息

CAS号	2421117-98-6	储存条件	粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C28H26N4O4S2	运输	蓝冰
分子量	546.66	别名

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