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Purity: ≥98%
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.
| ln Vitro |
In a DX2-dependent way, BC-DXI-843 (0.0316-31.6 μM; 72 hours) inhibits the growth of cancer cells. In A549 cells, the EC50 was 1.20 μM, which is comparable to the IC50 for DX2 inhibition. On WI-26 cells, however, no inhibitory impact was seen, indicating that BC-DXI-843 exclusively lowers cancer cell viability [1].
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| ln Vivo |
A tumor xenograft mouse model (using H460 cells) showed the in vivo efficacy of BC-DXI-843 (50 mg/kg; intraperitoneally; every other day for 15 days) [1].
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| Cell Assay |
Cell proliferation experiment [1]
Cell Types: A549 cancer cells and WI-26 normal cells Tested Concentrations: 0.0316, 0.1, 0.316, 1, 3.16, 10, 31.6 μM Incubation Duration: 72 hrs (hours) Experimental Results: EC50 in A549 cells is 1.20 μM. No inhibition of WI-26 cells was observed. |
| Animal Protocol |
Animal/Disease Models: 7weeks old female BALB/cSLC-nu/nu (nude) mice carrying H460 cell xenografts [1]
Doses: 50 mg/kg Route of Administration: intraperitoneally (ip) (ip); every other day for 15 days Experimental Results: After BC-DXI-843 administration, the embedded tumor volume gradually diminished, but the body weight did not change. The weight of the resected tumors diminished after the mice were sacrificed. |
| 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.
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| Molecular Formula |
C28H26N4O4S2
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|---|---|
| Molecular Weight |
546.66
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| Exact Mass |
546.1395
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| Elemental Analysis |
C, 61.52; H, 4.79; N, 10.25; O, 11.71; S, 11.73
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| CAS # |
2421117-98-6
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| Related CAS # |
2421117-98-6
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| SMILES |
O=C(NC1=NC(C2=CC=C(OC)C=C2)=CS1)[C@@H](NS(=O)(C3=CC=C(C)C=C3)=O)CC4=CNC5=C4C=CC=C5
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| InChi Key |
VLPGAOXBMXGNGM-VWLOTQADSA-N
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| InChi Code |
InChI=1S/C28H26N4O4S2/c1-18-7-13-22(14-8-18)38(34,35)32-25(15-20-16-29-24-6-4-3-5-23(20)24)27(33)31-28-30-26(17-37-28)19-9-11-21(36-2)12-10-19/h3-14,16-17,25,29,32H,15H2,1-2H3,(H,30,31,33)/t25-/m0/s1
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| Chemical Name |
(S)-3-(1H-Indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide
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| Synonyms |
BCDXI843 BCDXI-843 BCDXI 843 BC-DXI-843 BC-DXI843 BC-DXI 843
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~457.32 mM)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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