Description

Product Description

Brigatinib (CAS 1197953-54-0) is a next-generation small-molecule tyrosine kinase inhibitor (TKI) designed to target ALK fusion proteins and select EGFR mutations, including resistant variants. By inhibiting aberrant kinase activity, Brigatinib disrupts downstream signaling pathways such as PI3K/AKT and MAPK/ERK, leading to cell cycle arrest, apoptosis, and suppression of tumor cell proliferation.

Physical and Chemical Properties:

• Molecular formula: C29H39ClN7O2

• Molecular weight: 584.1 g/mol

• Appearance: White to off-white crystalline powder

• Solubility: Soluble in DMSO, ethanol; moderate aqueous solubility

• Stability: Stable at 2–8 °C; protect from light and moisture

Research Applications:

1. Kinase Signaling Studies: Evaluates ALK-driven and EGFR-mutant signaling pathways in cancer cell lines.

2. Apoptosis and Cell Cycle Research: Induces apoptosis via mitochondrial pathway and inhibits proliferation through G1/S or G2/M phase arrest.

3. Drug Resistance Modeling: Explores resistance mechanisms such as secondary ALK mutations, bypass signaling, and compensatory kinase activation.

4. Combination Therapy Studies: Used to test synergistic or additive effects with other chemotherapeutics, kinase inhibitors, or targeted agents.

5. In vivo Preclinical Models: Suitable for xenograft studies, pharmacokinetics, and pharmacodynamics of ALK/EGFR inhibition.

6. Mechanistic Investigations: Explores molecular determinants of sensitivity and resistance, transcriptional regulation, and downstream kinase signaling modulation.

Experimental Considerations:

• Handling: Powder should be handled with gloves, lab coat, and eye protection.

• Dosing: Experimental concentrations depend on cell type, assay design, and target sensitivity.

• Solvent Compatibility: Dissolve in DMSO or ethanol prior to dilution in culture media.

• Storage: Store at 2–8 °C; avoid freeze-thaw cycles; protect from light and moisture.

Brigatinib’s high selectivity, potent ALK/EGFR inhibition, and high purity (≥99%) make it a crucial reagent for preclinical kinase research, mechanistic studies, and evaluation of targeted therapy strategies.

Product Specifications

Mechanism of Action

Brigatinib is a potent, next-generation tyrosine kinase inhibitor (TKI) that selectively targets ALK (anaplastic lymphoma kinase) fusion proteins and specific EGFR mutations, including variants resistant to first- and second-generation inhibitors. By binding to the ATP-binding site of ALK and mutant EGFR, Brigatinib inhibits kinase activity, thereby disrupting downstream signaling pathways critical for cell survival, proliferation, and metastasis, such as PI3K/AKT, MAPK/ERK, and JAK/STAT.

Key Molecular Mechanisms:

1. ALK Inhibition: Blocks aberrant ALK signaling in ALK-positive tumor cells, reducing proliferation and triggering apoptotic pathways.

2. EGFR Mutant Targeting: Inhibits select EGFR mutations, including T790M, which confer resistance to earlier-generation inhibitors.

3. Cell Cycle Arrest: Induces G1/S or G2/M phase arrest via inhibition of cyclin-dependent kinases and restoration of checkpoint control.

4. Apoptosis Induction: Activates mitochondrial apoptotic pathways, caspases, and Bcl-2 family protein modulation.

5. Signal Transduction Modulation: Downregulates survival pathways and transcriptional programs promoting tumor growth.

6. Drug Resistance Research: Serves as a model to study secondary ALK mutations, compensatory kinase activation, and mechanisms of TKI resistance.

Experimental Applications:

• In vitro: Analysis of ALK/EGFR signaling inhibition, cell proliferation, apoptosis assays, and drug sensitivity/resistance profiling.

• In vivo: Xenograft models for preclinical evaluation of tumor growth inhibition, pharmacokinetics, pharmacodynamics, and molecular biomarker studies.

• Combination Therapy Research: Evaluates synergistic effects with other chemotherapeutics, TKIs, or targeted agents.

• Mechanistic Investigations: Studies intracellular signaling, downstream phosphorylation targets, transcriptional changes, and apoptosis biomarkers.

Brigatinib’s selectivity, high potency, and reliable kinase inhibition make it an essential reagent for preclinical targeted therapy studies, signaling pathway elucidation, and resistance mechanism research.

Side Effects

Brigatinib is a research-grade compound; laboratory handling requires standard safety precautions:

• Cytotoxicity: Induces apoptosis and inhibits proliferation in sensitive tumor cell lines; effects are concentration- and time-dependent.

• Handling Safety:

  • Use gloves, lab coat, and eye protection.

  • Handle in biosafety cabinets if dust or aerosol formation is possible.

• Storage: Store at 2–8 °C; protect from light and moisture; avoid repeated freeze-thaw cycles.

• Environmental Safety: Dispose of residual powder and contaminated materials according to institutional safety protocols.

Experimental Observations:

• In vitro: ALK/EGFR signaling inhibition, cell cycle arrest, apoptosis activation, altered downstream kinase phosphorylation.

• In vivo: Tumor growth suppression, pharmacodynamic effects on ALK/EGFR targets, biomarker modulation.

Keywords

Brigatinib, CAS 1197953-54-0, ALK inhibitor, EGFR TKI, tyrosine kinase inhibitor, apoptosis induction, cell cycle arrest, targeted therapy research, kinase signaling, high purity, ≥99% purity, factory peptide/small-molecule supplier, peptide wholesale China, China peptide manufacturer, OEM & bulk peptide production.

Shipping Guarantee

All Brigatinib Brigatinib shipments are handled via validated cold-chain logistics to maintain chemical stability and potency. The powder is sealed in light- and moisture-protected containers with secondary packaging. Full tracking, insurance coverage, and international courier support ensure secure delivery.

Trade Assurance

Brigatinib authenticity is guaranteed, with ≥99% purity verified by HPLC, MS, and NMR. Each batch includes a Certificate of Analysis (CoA). Trade assurance covers replacement or refund for deviations from listed specifications, ensuring reliable, high-purity product for preclinical research.

Payment Support

Secure global payment options: PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are encrypted and verified for confidentiality and fund protection.

Disclaimer

This Brigatinib product is intended for laboratory research use only. It is not for human or veterinary administration. Researchers must follow institutional safety protocols. Data generated with Brigatinib should not be interpreted as clinical or therapeutic guidance.

References

1. PubChem: Brigatinib (CID 24826730)  ↗

2. ChEMBL: Brigatinib Bioactivity (ChEMBL ID CHEMBL3543824)  ↗

3. DrugBank: Brigatinib – DB11706  ↗

4. PubMed ID 26058674 – Brigatinib preclinical evaluation and mechanism  ↗

5. IUPHAR/BPS Guide to Pharmacology: ALK inhibitors  ↗