Brigimadlin
Based on 1 Customer Validation
Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 2095116-40-6
- Formula: C31H25Cl2FN4O3
- Molecular Weight:591.46
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Brigimadlin (0-10 nM, 48 h) inhibits viability and induces cell death in brain tumor stem cells (BTSCs)[3].
Brigimadlin (1-50 nM, 48 h) induces apoptosis and increases p53 transcriptional targets (p21 and PUMA) in BT48, BT67, BT73 cells[3].
Brigimadlin (1 nM, 48 h) disrupts the interaction between MDM2 and wild-type p53 in brain tumor stem cells (BTSCs)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:BT48, BT50, BT67, BT69, BT89, BT94
-
Concentration:0-10 nM
-
Incubation Time:48 h
-
Result:IC50: 58.5, 21.1, 37.9, 89.8, 16.7, 46.8 pM.
-
Cell Line:BT48, BT67, BT73 cells
-
Concentration:0-50 nM
-
Incubation Time:48 h
-
Result:Upregulated p21 and PUMA, and increased cleaved PARP level.
Brigimadlin (50 mg/kg, p.o., a single dose) increasees PD biomarkers (CDKN1a and GDF15) in the brain in orthotopic GBM-derived BTSC models (BT48 and BT67) in SCID mice, and has low systemic clearance[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2095116-40-6
-
Appearance Solid
-
Molecular Weight 591.46
-
Formula C31H25Cl2FN4O3
-
Color White to off-white
-
SMILES
OC(C1=C(C)C2=NN([C@@]([C@]3([H])C4)([H])[C@H](C5=C(C(Cl)=CC=C5)F)[C@@]6(C7=CC=C(Cl)C=C7NC6=O)N3CC8CC8)C4=C2C=C1)=O
-
Synonyms
BI 907828
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (84.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.11 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
-
Handling Instructions (2659 KB)
References
[2]. WHO Drug Information-World Health Organization (WHO).
[3]. Hao X, et al. BI-907828, a novel potent MDM2 inhibitor, inhibits glioblastoma brain tumor stem cells in vitro and prolongs survival in orthotopic xenograft mouse models. Neuro Oncol. 2023 May 4;25(5):913-926. [Content Brief]
[4]. Yoo C, et al. Brightline-2: a phase IIa/IIb trial of brigimadlin (BI 907828) in advanced biliary tract cancer, pancreatic ductal adenocarcinoma or other solid tumors. Future Oncol. 2024 Jan 12. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6907 mL | 8.4537 mL | 16.9073 mL | 42.2683 mL |
| 5 mM | 0.3381 mL | 1.6907 mL | 3.3815 mL | 8.4537 mL | |
| 10 mM | 0.1691 mL | 0.8454 mL | 1.6907 mL | 4.2268 mL | |
| 15 mM | 0.1127 mL | 0.5636 mL | 1.1272 mL | 2.8179 mL | |
| 20 mM | 0.0845 mL | 0.4227 mL | 0.8454 mL | 2.1134 mL | |
| 25 mM | 0.0676 mL | 0.3381 mL | 0.6763 mL | 1.6907 mL | |
| 30 mM | 0.0564 mL | 0.2818 mL | 0.5636 mL | 1.4089 mL | |
| 40 mM | 0.0423 mL | 0.2113 mL | 0.4227 mL | 1.0567 mL | |
| 50 mM | 0.0338 mL | 0.1691 mL | 0.3381 mL | 0.8454 mL | |
| 60 mM | 0.0282 mL | 0.1409 mL | 0.2818 mL | 0.7045 mL | |
| 80 mM | 0.0211 mL | 0.1057 mL | 0.2113 mL | 0.5284 mL |
Powered by Bioz