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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.

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BC-DXI-843 Chemical Structure

BC-DXI-843 Chemical Structure

CAS No. : 2421117-98-6

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5 mg USD 115 In-stock
10 mg USD 190 In-stock
25 mg USD 350 In-stock
50 mg USD 530 In-stock
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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]

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: 20d; BC-DXI-843
Inhibition of nanoluciferase-tagged AIMP2 (unknown origin) expressed in human A549 cells measured after 4 hrs by luminescence assay
Inhibition of nanoluciferase-tagged AIMP2 (unknown origin) expressed in human A549 cells measured after 4 hrs by luminescence assay
[PMID: 32315177]
A549 IC50
0.92 μM
Compound: 20d; BC-DXI-843
Inhibition of nanoluciferase-tagged AIMP2 DX2 isoform (unknown origin) expressed in human A549 cells measured after 4 hrs by luminescence assay
Inhibition of nanoluciferase-tagged AIMP2 DX2 isoform (unknown origin) expressed in human A549 cells measured after 4 hrs by luminescence assay
[PMID: 32315177]
A549 EC50
1.2 μM
Compound: 20d; BC-DXI-843
Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay
[PMID: 32315177]
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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) 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.
Molecular Weight

546.66

Formula

C28H26N4O4S2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC(C=C1)=CC=C1C2=CSC(NC([C@@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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (457.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8293 mL 9.1465 mL 18.2929 mL 45.7323 mL
5 mM 0.3659 mL 1.8293 mL 3.6586 mL 9.1465 mL
10 mM 0.1829 mL 0.9146 mL 1.8293 mL 4.5732 mL
15 mM 0.1220 mL 0.6098 mL 1.2195 mL 3.0488 mL
20 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2866 mL
25 mM 0.0732 mL 0.3659 mL 0.7317 mL 1.8293 mL
30 mM 0.0610 mL 0.3049 mL 0.6098 mL 1.5244 mL
40 mM 0.0457 mL 0.2287 mL 0.4573 mL 1.1433 mL
50 mM 0.0366 mL 0.1829 mL 0.3659 mL 0.9146 mL
60 mM 0.0305 mL 0.1524 mL 0.3049 mL 0.7622 mL
80 mM 0.0229 mL 0.1143 mL 0.2287 mL 0.5717 mL
100 mM 0.0183 mL 0.0915 mL 0.1829 mL 0.4573 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BC-DXI-843
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HY-136431
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