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BC-DXI-843 

Cat. No.: HY-136431
Handling Instructions

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.

For research use only. We do not sell to patients.

BC-DXI-843 Chemical Structure

BC-DXI-843 Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

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]

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].

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.
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.
Molecular Weight

546.66

Formula

C₂₈H₂₆N₄O₄S₂

SMILES

COC(C=C1)=CC=C1C2=CSC(NC([[email protected]@H](NS(C3=CC=C(C)C=C3)(=O)=O)CC4=CNC5=C4C=CC=C5)=O)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BC-DXI-843OthersAIMP2-DX2lungcancerA549Inhibitorinhibitorinhibit

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Product name:
BC-DXI-843
Cat. No.:
HY-136431
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