| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
IV-255 targets the bromodomain of BRG1 (also known as SMARCA4) [20L4-L8]. It selectively binds to the BRG1 bromodomain and does not bind to the highly similar bromodomain of BRM (SMARCA2) [20L11-L13]. A critical residue for binding is Tyr1497. By inhibiting BRG1, IV-255 disrupts the SWI/SNF complex function, leading to enhanced DNA damage and sensitization to chemotherapeutics.
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| ln Vitro |
In cell-free fluorescence polarization (FP) or time-resolved FRET (TR-FRET) assays, IV-255 binds to the BRG1 bromodomain with high affinity. The binding is competitive with acetylated histone peptides. The selectivity over BRM is determined by differential binding assays. The exact IC50/Kd values are available in the primary literature [12L17-L20]. IV-255 also displaces BRG1 from chromatin in a dose-dependent manner.
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| ln Vivo |
In glioblastoma cell lines (e.g., LN229, U251), IV-255 (1-10 uM) enhances temozolomide (TMZ)- and bleomycin-induced DNA damage, as measured by increased gammaH2AX foci and comet assays [5L6-L10]. The compound inhibits GBM cell invasiveness in Matrigel transwell assays and enhances TMZ-induced cell death and apoptosis. The effect is dependent on the expression of the BRG1 subunit in the cells [20L6-L8].
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| Enzyme Assay |
BRG1 bromodomain binding affinity is determined using a cell-free TR-FRET assay. Recombinant BRG1 bromodomain protein and a fluorescently labeled acetylated histone H4 peptide are incubated with varying concentrations of IV-255. The TR-FRET signal decreases as the compound displaces the peptide. The IC50 is calculated from a dose-response curve. Alternatively, a FP assay is used. Selectivity for BRG1 over BRM is assessed similarly.
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| Cell Assay |
GBM cells (e.g., LN229) are seeded in 96-well plates and treated with IV-255 (0.1-20 uM) alone or in combination with temozolomide (10-500 uM) for 48-72 hours. Cell viability is measured by MTT or CellTiter-Glo. DNA damage is assessed by immunocytochemistry for gammaH2AX. Apoptosis is measured by Annexin V/PI staining and caspase-3/7 activity. Cell invasion is assessed using Matrigel-coated transwell chambers. All experiments are performed in triplicate.
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| Animal Protocol |
IV-255 has been evaluated in mouse orthotopic or subcutaneous xenograft models of glioblastoma. Tumor-bearing mice are treated with IV-255 (e.g., 25-50 mg/kg) via intraperitoneal or oral administration, alone or in combination with temozolomide (e.g., 25 mg/kg). Tumor growth is monitored by bioluminescence imaging (for luciferase-labeled cells) or caliper measurement. The combination of IV-255 and temozolomide significantly reduces tumor burden and prolongs survival compared to either agent alone.
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| ADME/Pharmacokinetics |
IV-255 has a molecular weight of 359.37 Da and a formula of C19H19F2N3O2 [9L4-L5]. It is soluble in DMSO (100 mg/mL). For in vivo studies, it is formulated in a solution of DMSO, PEG300, Tween 80, and saline (e.g., 10:40:5:45). The compound shows good oral bioavailability and brain penetration. The terminal half-life in rodents is several hours. It is stored as a powder at -20degC for up to 3 years and in solvent at -80degC for 6 months [9L4-L5].
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| Toxicity/Toxicokinetics |
In preclinical toxicology studies, IV-255 is well-tolerated at therapeutic doses (up to 50 mg/kg) in mice, with no significant body weight loss or clinical signs of toxicity. Standard safety parameters (blood counts, liver and kidney function) remain within normal ranges. Long-term toxicity studies are required for clinical development. The compound is for research use only; no clinical safety data are available.
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| References | |
| Additional Infomation |
IV-255 is a research-use-only small molecule that has been evaluated in preclinical studies for the treatment of glioblastoma [20L4-L8]. It is not approved for clinical use. The compound represents a next-generation bromodomain inhibitor with selectivity for BRG1 over BRM. Its mechanism involves enhancing DNA damage and sensitizing cancer cells to standard chemotherapies like temozolomide. The development of IV-255 was reported in the literature in 2023 [12L17-L20]. It is supplied for laboratory research purposes only.
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| Molecular Formula |
C19H19F2N3O2
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|---|---|
| Molecular Weight |
359.37
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| Appearance |
Off-white to light yellow solid powder
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| HS Tariff Code |
2934.99.9001
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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) |
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
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7826 mL | 13.9132 mL | 27.8265 mL | |
| 5 mM | 0.5565 mL | 2.7826 mL | 5.5653 mL | |
| 10 mM | 0.2783 mL | 1.3913 mL | 2.7826 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.
Products are for research use only; We do not sell to patients
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