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BC-DXI-843 is inhibitor of AIMP2-DX2, and is potential for development of novel therapeutics targeting AIMP2-DX2 in lung cancer.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $35 | In Stock | In Stock | |
| 5 mg | $56 | In Stock | In Stock | |
| 10 mg | $93 | In Stock | In Stock | |
| 25 mg | $173 | In Stock | In Stock | |
| 50 mg | $260 | In Stock | In Stock | |
| 100 mg | $381 | In Stock | In Stock | |
| 200 mg | $542 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $68 | In Stock | In Stock |
| Description | BC-DXI-843 is inhibitor of AIMP2-DX2, and is potential for development of novel therapeutics targeting AIMP2-DX2 in lung cancer. |
| Targets&IC50 | AIMP2-DX2:0.92 μM (IC50), AIMP2:IC50 >100 μM |
| In vitro | Optimization of hit BC-DXI-04 (IC50 = 40.1 μM) provided new potent sulfonamide based AIMP2-DX2 inhibitors.?Among these, BC-DXI-843 showed improved inhibition against AIMP2-DX2 (IC50 = 0.92 μM) with more than 100-fold selectivity over AIMP2 in a luciferase assay.?Several binding assays indicated that this compound effectively induces cancer cell apoptosis by specifically interrupting the interaction between DX2 and HSP70, which leads to the degradation of DX2 via Siah1-mediated ubiquitination. |
| In vivo | 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. |
| Molecular Weight | 546.66 |
| Formula | C28H26N4O4S2 |
| Cas No. | 2421117-98-6 |
| Smiles | COc1ccc(cc1)-c1csc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NS(=O)(=O)c2ccc(C)cc2)n1 |
| Relative Density. | 1.381 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 245 mg/mL (448.18 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.15 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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