BRD4-IN-12 |
Catalog No.GC79143
One-Click Copy Product Info
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BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3112325-99-9
Sample solution is provided at 25 µL, 10mM.
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In Vivo, BRD4-IN-12 (H5) (25 mg/kg or 50 mg/kg; p.o.; once a day; for 18 days) exhibits 52% and 82% tumor growth inhibition (TGI) at 25 mg/kg and 50 mg/kg, respectively, in male BALB/c nude mice bearing HCT-116 colorectal cancer xenografts; maintains stable body weight and causes no significant pathological damage to major organs (heart, liver, spleen, lung, kidney); and downregulates the expression of c-MYC and BCL-2 in tumor tissues; induces increased cell spacing, smaller and rounded nuclei in tumor tissues of male BALB/c nude mice with HCT-116 colorectal cancer xenografts[1].
In Vitro, BRD4-IN-12 (H5) (72 h) shows cytotoxicity against HCT-116 colorectal cancer cells with an IC50 value of 0.84 μM, the cytotoxicity of BRD4-IN-12 induced in HCT-116 cells is BRD4-dependent[1]. BRD4-IN-12 (1.25-5.0 μM; 24 h) downregulates the protein expression of c-MYC, CDK4 and BCL-2, and dose-dependently upregulates the protein expression of p21 in HCT-116 cells[1]. BRD4-IN-12 (20 μM; 3 h) stabilizes BRD4 protein in HCT-116 cell lysates, confirming its intracellular binding to BRD4[1].
References:
[1]. Fang Z, et al. Discovery of an orally bioavailable pyridone-based BRD4 inhibitor with potent antitumor efficacy in colorectal cancer. Eur J Med Chem. 2026 Mar 5;305: 18573.
| Cas No. | 3112325-99-9 | SDF | |
| Formula | C21H24N4O4S | M.Wt | 428.5 |
| Solubility | Storage | Store at -20°C | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3337 mL | 11.6686 mL | 23.3372 mL |
| 5 mM | 466.7 μL | 2.3337 mL | 4.6674 mL |
| 10 mM | 233.4 μL | 1.1669 mL | 2.3337 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)