MedChemExpress - Model Brigimadlin -2095116-40-6
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[1][2][3][4].MCE products for research use only. We do not sell to patients.
Brigimadlin
MCE China：Brigimadlin
Brand：MedChemExpress (MCE)
Cat. No.HY-152859
CAS：2095116-40-6
Synonyms：BI 907828
Purity：99.72%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
In Vitro：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].
In Vivo：Brigimadlin (15 and 50 mg/kg, p.o., once a week) inhibits tumor growth and increases median survival in orthotopic xenografts of both a MDM2 amplified (BT48) and a normal CN (BT67), TP53 wild-type BTSC model[3]. Brigimadlin (50 mg/kg, p.o., a single dose) increasees PD biomarkers (CDKN1a and GDF15) in the brain in orthotopic GBM patient-derived BTSC models (BT48 and BT67) in SCID mice, and has low systemic clearance[3].
Hot selling product：Navoximod | TLR7/8 agonist 1 | Tolebrutinib | Ricolinostat | Valsartan | Novobiocin (sodium) | Bixin | Pilocarpine | Cinnabarinic acid | Kanamycin (sulfate)
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
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]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。