Apoptosis/necrosis inducer 1 (compound 1F) (24–72 hours) showed concentration- and time-dependent antiproliferative activity against U87 glioblastoma cells, with IC50 values of 6.87 μM (24 hours), 3.85 μM (48 hours), and 3.68 μM (72 hours), respectively [1]. Apoptosis/necrosis inducer 1 (24–72 hours) showed stable antiproliferative activity against U251 glioblastoma cells, with IC50 values ranging from 5.28 to 5.90 μM over 24, 48, and 72 hours [1]. Apoptosis/necrosis inducer 1 (2–8 μM; 48 hours) inhibited DNA synthesis in U87 glioblastoma cells in a dose-dependent manner [1]. Apoptosis/necrosis inducer 1 (3-9 μM; 48 h) dose-dependently inhibited DNA synthesis in U251 glioblastoma cells [1]. Apoptosis/necrosis inducer 1 (2-8 μM; 12 h) dose-dependently inhibited the migration of U87 and U251 glioblastoma cells [1]. Apoptosis/necrosis inducer 1 (2-8 μM; 19 h) dose-dependently inhibited the invasion of U87 and U251 glioblastoma cells [1]. Apoptosis/necrosis inducer 1 (2-8 μM; 48 h) decreased the mitochondrial membrane potential of U87 glioblastoma cells [1]. Apoptosis/necrosis inducer 1 (3-9 μM; 48 h) decreased the mitochondrial membrane potential of U251 glioblastoma cells [1]. Apoptosis/necrosis inducer 1 (2-8 μM; 48 h) can increase the level of reactive oxygen species in U87 glioblastoma cells[1]. Apoptosis/necrosis inducer 1 (3-9 μM; 48 h) can increase the level of reactive oxygen species in U251 glioblastoma cells[1]. Apoptosis/necrosis inducer 1 (2-8 μM; 48 h) can induce G2/M phase cell cycle arrest in U87 glioblastoma cells[1]. Apoptosis/necrosis inducer 1 (3-9 μM; 48 h) can induce G1/G0 phase cell cycle arrest in U251 glioblastoma cells[1]. Apoptosis/necrosis inducer 1 (2-8 μM; 48 h) can induce apoptosis in U87 glioblastoma cells[1]. Apoptosis/necrosis inducer 1 (3-9 μM; 48 h) can induce apoptosis in U251 glioblastoma cells[1]. Apoptosis/necrosis inducer 1 (2-8 μM; 48 h) can regulate the expression of apoptosis-related proteins in U87 glioblastoma cells (decreasing the expression of Caspase 9, Caspase 3 and Bcl-2; increasing the expression of BAX and Cleaved Caspase 8)[1]. Apoptosis/necrosis inducer 1 (2-9 μM; 48 h) triggers necroptosis in U87 and U251 glioblastoma cells by coordinating the regulation of the TNF-α/NF-κB/MAPK signaling pathway[1].

Apoptosis/necrosis inducer 1 (compound 1f) (50-200 mg/kg; orally; daily; 21 days) inhibited GL261 tumor growth and improved survival in orthotopic GBM mice [1]. Apoptosis/necrosis inducer 1 (compound 1F) (100 mg/kg; by gavage; single dose) showed good blood-brain barrier permeability in healthy BALB/c mice [1].

Cell migration assay [1]
Cell Types: U87 and U251 glioblastoma cells
Tested Concentrations: 2, 4, 8 μM
Incubation Duration: 12 hours
Experimental Results: Compared with the control group, the number of migrating cells decreased in a dose-dependent manner.

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Cell invasion assay [1]
Cell Types: U87 glioblastoma cells
Tested Concentrations: 2, 4, 8 μM
Incubation Duration: 19 hours
Experimental Results: Compared with the control group, the number of invading cells was reduced in a dose-dependent manner.

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Cell invasion assay [1]
Cell Types: U251 glioblastoma cells
Tested Concentrations: 3, 6, 9 μM
Incubation Duration: 19 hours
Experimental Results: Compared with the control group, the number of invading cells was reduced in a dose-dependent manner.

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Cell cycle analysis [1]
Cell Types: U87 glioblastoma cells
Tested Concentrations: 2, 4, 8 μM
Incubation Duration: 48 hours
Experimental Results: After high concentration treatment, the proportion of cells in the G2/M phase increased from 10.9% to 19.6%, and the proportion of cells in the G1/G0 phase decreased from 61.9% to 51.6%.

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Cell cycle analysis [1]
Cell Types: U251 glioblastoma cells
Tested Concentrations: 3, 6, 9 μM
Incubation Duration: 48 hours
Experimental Results: High concentration treatment induced G1/G0 phase arrest.

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Apoptosis analysis [1]
Cell Types: U87 glioblastoma cells
Tested Concentrations: 2, 4, 8 μM
Incubation Duration: 48 hours
Experimental Results: Compared with the control group, the percentage of early and late apoptosis was increased.

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Apoptosis analysis [1]
Cell Types: U251 glioblastoma cells
Tested Concentrations: 3, 6, 9 μM
Incubation Duration: 48 hours
Experimental Results: Compared with the control group, the percentage of early and late apoptosis was increased.

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Western Blot Analysis [1]
Cell Types: U87 glioblastoma cells
Tested Concentrations: 2, 4, 8 μM
Incubation Duration: 48 hours
Experimental Results: Caspase 9, Caspase 3 and Bcl-2 protein levels decreased; BAX and Cleaved Caspase 8 expression increased.

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Western Blot Analysis [1]
Cell Types: U87 and U251 glioblastoma cells
Tested Concentrations: 2, 4, 8 μM (U87), 3, 6, 9 μM (U251)
Incubation Duration: 48 hours
Experimental Results: Phosphorylation of RIP1 Ser166, RIP3 Ser227 and MLKL Ser358 was significantly upregulated in U87 and U251 cells.

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Animal/Disease Models:BALB/c (male, specific pathogen clearance grade, orthotopic GL261-Luc glioblastoma model) [1]
Doses: 50, 100, 200 mg/kg
Route of Administration: Oral; daily; 21 days
Experimental Results: The relative fluorescence intensity of the tumor was significantly reduced on day 21; the survival time was prolonged in the 100 mg/kg dose group.

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Animal/Disease Models:BALB/c (male, SPF grade) [1]
Doses: 100 mg/kg
Route of Administration: Gavage; single dose
Experimental Results: Average brain tissue concentration reached 261.30 ng/g

[1]. Sinomenine derivative 1f suppresses glioblastoma through inducing both apoptosis mediated by intrinsic pathway and necroptosis mediated by TNF-α/NF-κB/MAPK signaling pathway. Eur J Med Chem. 2026 Feb 15;304:118535.

C33H51NO5

541.76

Typically exists as solids at room temperature

CCCCCCCCCCCCCC(OC(C(OC)=CC=C1C[C@H]2C3C[C@H]4OC)=C1[C@]3(CCN2C)CC4=O)=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.)