Anti-non-small cell lung cancer drug-2 (compound 6o) (10-160 nM; 48 h) effectively inhibited the proliferation of A549, H1299, H2030, H1975, A549/T and A549/CDDP non-small cell lung cancer cell lines, with IC50 values ranging from 1.54 nM to 11.72 nM, and showed no significant toxicity to normal human umbilical vein endothelial cells (HUVECs) at effective tumor-inhibiting concentrations [1]. Anti-non-small cell lung cancer drug-2 (compound 6o) (100 μM; 2.5 h) caused A549 cells to release 10.02 μM of nitric oxide [1]. Anti-non-small cell lung cancer drug-2 (50 nM; 48 h) had anti-proliferative activity in A549 and A549/CDDP cells, which was nitric oxide-dependent and concentration-dependent reversal could be achieved through hemoglobin clearance [1]. Anti-non-small cell lung cancer drug-2 (100 nM; 48 h) exhibits anti-proliferative activity in A549 and A549/CDDP cells, an activity dependent on ferroptosis that can be concentration-dependently reversed by Ferrostatin-1 [1]. Anti-non-small cell lung cancer drug-2 (specific concentration; 4 h) dose-dependently increases the accumulation of ferrous ions in A549 and A549/CDDP cells, thereby supporting the induction of ferroptosis [1]. Anti-non-small cell lung cancer drug-2 (specific concentration; 4 h) dose-dependently induces lipid peroxidation in A549 and A549/CDDP cells, with green/red fluorescence ratios increasing to 1.51 and 1.10, respectively [1]. Anti-non-small cell lung cancer drug-2 (15-60 nM; 12 h) dose-dependently downregulated the expression of SLC7A11 and GPX4 proteins in A549 and A549/CDDP cells via an ferroptosis-dependent mechanism [1]. Anti-non-small cell lung cancer drug-2 (20-80 nM; 3-12 h) dose- and time-dependently increased the level of reactive oxygen species in A549 and A549/CDDP cells [1]. Anti-non-small cell lung cancer drug-2 (40-80 nM; 12 h) dose-dependently depleted glutathione in A549 and A549/CDDP cells and decreased the GSH/GSSG ratio, thereby disrupting redox homeostasis [1]. Anti-non-small cell lung cancer drug-2 (20–80 nM; 4 hours) increased mitochondrial nitric oxide levels in A549 (20 nM) and A549/CDDP (80 nM) cells[1]. Anti-non-small cell lung cancer drug-2 (specific concentration; 4 hours) dose-dependently induced mitochondrial membrane potential collapse in A549 and A549/CDDP cells[1]. Anti-non-small cell lung cancer drug-2 (specific concentration; 4 hours) dose-dependently increased mitochondrial reactive oxygen species (superoxide) levels in A549 and A549/CDDP cells[1].

Anti-non-small cell lung cancer drug-2 (compound 6o) (5-10 mg/kg; intravenous injection; every 2 days; 20 days) showed dose-dependent in vivo antiproliferative activity against cisplatin-resistant A549/CDDP xenografts, with 10 mg/kg being more effective than 10 mg/kg of cisplatin, while maintaining good safety and no organ toxicity was observed [1].

Animal/Disease Models:Nude mice (female, SPF grade, xenograft model of cisplatin-resistant non-small cell lung cancer) [1]
Doses: 5 mg/kg; 10 mg/kg
Route of Administration: Intravenous injection (tail vein); once every 2 days; for 20 days
Experimental Results: Compared with the vector control group, the tumor volume of the 5 mg/kg dose group was significantly reduced. Compared with the vector control group and the 10 mg/kg cisplatin group, the final tumor weight of the 5 mg/kg dose group was significantly reduced. The 10 mg/kg dose group had the largest reduction in tumor volume among all treatment groups. The final tumor weight of the 10 mg/kg dose group was significantly lower than that of the vector control group and the 10 mg/kg cisplatin group. No significant weight loss or behavioral abnormalities were observed in either dose group. No histopathological damage to the heart, liver, spleen, lungs and kidneys was found by H&E staining.

[1]. Novel Hybrids of 3-Substituted Coumarin and Phenylsulfonylfuroxan as Potent Antitumor Agents against Wild-Type and Drug-Resistant Nonsmall Cell Lung Cancer Cell Lines. J Med Chem. 2026;69(6):7238-7261.

C27H20CL2N2O8S

603.43

3063042-21-4

Typically exists as solids at room temperature

O=S(C1=[N+]([O-])ON=C1OCCOC2=CC(O3)=C(C=C2)C(C)=C(CC4=CC(Cl)=CC(Cl)=C4)C3=O)(C5=CC=CC=C5)=O

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)