Anticancer agent 296 (compound 5b) (1.25-10 μM; 48 h) can effectively inhibit the proliferation of A549 and HeLa cancer cells, with IC50 values of 3.88 μM and 3.89 μM, respectively, and has good safety for normal cells [1]. Anticancer agent 296 (1.94-3.88 μM; 48 h; mitomycin C pretreatment for 24 h) can effectively inhibit the migration of A549 cells in a concentration-dependent manner, and the concentration of 3.88 μM can reduce the wound healing rate to 8.19% [1]. Anticancer drug 296 (1.94-7.76 μM; 24 h) can downregulate the expression of FAK protein in A549 cells, thereby inhibiting cell migration, and activate the PERK-eIF2α-CHOP endoplasmic reticulum stress pathway and endogenous apoptosis pathway in A549 cells by regulating key proteins [1]. The anticancer drug 296 (1.94-7.76 μM; 7 days) can effectively inhibit the colony formation of A549 cells at a concentration ≥3.88 μM[1]. The anticancer drug 296 (1.94-7.76 μM; 24 h) can activate autophagy in A549 cells by upregulating Beclin-1 and promoting LC3 I/II conversion[1]. The anticancer drug 296 (1.94-7.76 μM; 24 h) induces S-phase arrest in A549 cells in a dose-dependent manner, and the 7.76 μM drug increases the proportion of S-phase cells to 31.33% by downregulating cell cycle-related proteins[1]. The anticancer drug 296 (1.94-7.76 μM; 24 h) reduces the mitochondrial membrane potential of A549 cells in a concentration-dependent manner[1]. The anticancer drug 296 (1.94–7.76 μM; 24 h) increased the level of reactive oxygen species (ROS) in A549 cells[1]. The anticancer drug 296 (3.88–7.76 μM; 24 h) induced oxidative stress in A549 cells by decreasing glutathione (GSH) levels and increasing malondialdehyde (MDA) levels[1]. The anticancer drug 296 (1.94–7.76 μM; 24 h) increased the intracellular calcium ion concentration in A549 cells, with 7.76 μM increasing the calcium ion concentration by 1.68-fold[1]. The anticancer drug 296 (3.88 μM; 24 h) induced endoplasmic reticulum stress in A549 cells through the PERK pathway, manifested as endoplasmic reticulum vacuolation[1]. The anticancer drug 296 (1.94-7.76 μM; 24 h) can induce early apoptosis in A549 cells, of which 7.76 μM can increase the early apoptosis rate to 11.14%[1].

Anticancer agent 296 (compound 5b) (10-20 mg/kg; intraperitoneal injection; daily; for 12 consecutive days) showed dose-dependent antitumor efficacy in A549 xenograft mice, with a tumor inhibition rate of 80.32% at 20 mg/kg [1].

Animal/Disease Models:BALB/c nude mice injected with A549 cells [1]
Doses: 10 mg/kg; 20 mg/kg
Route of Administration: Intraperitoneal injection; once daily for 12 consecutive days
Experimental Results: Tumor inhibition rates were 62.92% (10 mg/kg) and 80.32% (20 mg/kg), respectively. Induction of tumor cell DNA damage was achieved, with γH2AX positivity rates of 60.2% (10 mg/kg) and 69.3% (20 mg/kg), respectively. Inhibition of tumor proliferation was achieved, with Ki67 positivity rates of 36.5% (10 mg/kg) and 24.4% (20 mg/kg), respectively. No significant changes in body weight or chronic organ damage were observed.

[1]. Design, synthesis, and evaluation of unsymmetrical trifluoromethyl-containing bisindolylmethane derivatives inducing endoplasmic reticulum stress in human lung adenocarcinoma. Eur J Med Chem. 2026;305:118564.

C24H22BRF3N2OSI

519.43

Typically exists as solids at room temperature

COC1=CC=CC2=C1C(C(C3=CNC4=CC=C(C=C43)Br)(C(F)(F)F)C#C[Si](C)(C)C)=CN2

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.)