| Identification | Back Directory | [Name]
BC-DXI-843 | [CAS]
2421117-98-6 | [Synonyms]
BC-DXI-843
BC-Dxl-843
Inhibitor,lung,A549,BCDXI843,AIMP2-DX2,cancer,inhibit,BC DXI 843
(S)-3-(1H-Indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide
1H-Indole-3-propanamide, N-[4-(4-methoxyphenyl)-2-thiazolyl]-α-[[(4-methylphenyl)sulfonyl]amino]-, (αS)- | [Molecular Formula]
C28H26N4O4S2 | [MDL Number]
MFCD32693926 | [MOL File]
2421117-98-6.mol | [Molecular Weight]
546.66 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | 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. |
| [References]
[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. DOI:10.1021/acs.jmedchem.9b01961 |
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