Description

Product Description

Orelabrutinib (CAS 1655504-04-3) is a potent, covalent, selective inhibitor of Bruton’s tyrosine kinase (BTK), a critical enzyme in B-cell receptor (BCR) signaling and adaptive immune responses. Its specificity and efficacy make it a valuable tool for preclinical research investigating B-cell-mediated autoimmune disorders, hematologic malignancies, and related intracellular signaling networks.

In laboratory research, Orelabrutinib binds covalently to the cysteine-481 residue within the ATP-binding site of BTK, irreversibly inhibiting its kinase activity. This blockade prevents downstream phosphorylation of key substrates, including PLCγ2, BLNK, and NF-κB, ultimately modulating B-cell activation, proliferation, and survival. Researchers employ Orelabrutinib to dissect signaling pathways involved in autoimmune responses, lymphoma cell proliferation, and the modulation of cytokine release.

Orelabrutinib’s high selectivity over other kinases reduces off-target effects, allowing precise mechanistic studies in both in vitro and in vivo preclinical models. Its activity has been validated in various cellular assays, including B-cell lines, primary human B-cells, and murine models of autoimmune disease. By providing a controlled inhibition of BTK signaling, Orelabrutinib facilitates the study of molecular mechanisms underlying B-cell receptor engagement, downstream transcriptional regulation, and feedback control within immune networks.

The compound is supplied as a high-purity crystalline powder (≥99%) suitable for laboratory use. It is soluble in DMSO and ethanol, allowing for preparation of stock solutions for cell-based assays or animal studies. Rigorous quality control, including HPLC, mass spectrometry (MS), and nuclear magnetic resonance (NMR) verification, ensures batch consistency and reproducibility in mechanistic research.

Preclinical studies leveraging Orelabrutinib focus on elucidating B-cell activation, survival, and signaling crosstalk with other immune pathways. Its use in combination studies enables evaluation of synergistic or antagonistic interactions with other kinase inhibitors, immunomodulatory agents, or receptor antagonists. Researchers can investigate the temporal dynamics of BTK inhibition, downstream gene expression, and cellular adaptation in both normal and malignant B-cell populations.

Orelabrutinib’s role extends to mapping resistance mechanisms in B-cell malignancies, including mutations in BTK or downstream signaling effectors. It is also employed to study adaptive immune modulation in autoimmune disease models, including rheumatoid arthritis and systemic lupus erythematosus. The compound’s potency, selectivity, and high purity render it an indispensable reagent for mechanistic and translational research in B-cell biology.

Product Specifications 

Mechanism of Action

Orelabrutinib functions as a covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK). BTK plays a central role in B-cell receptor (BCR) signaling, mediating the phosphorylation of downstream targets such as PLCγ2, BLNK, and components of the NF-κB pathway.

By covalently binding to the cysteine-481 residue in BTK’s ATP-binding site, Orelabrutinib blocks kinase activity, preventing downstream phosphorylation events that drive B-cell activation, proliferation, and survival. This inhibition allows researchers to study the molecular mechanisms of B-cell-mediated autoimmune disorders, lymphoma progression, and signaling network adaptations.

In preclinical models, Orelabrutinib has been used to investigate:

• B-cell receptor signaling dynamics and transcriptional regulation.

• Cytokine release and immune response modulation.

• Adaptive resistance mechanisms arising from BTK mutations or pathway feedback.

• Combination effects with other kinase inhibitors or immunomodulatory compounds.

Its high selectivity reduces off-target kinase interactions, providing precise mechanistic insights into BTK-dependent pathways.

Side Effects

In a laboratory context, Orelabrutinib should be handled with care:

• Avoid inhalation, ingestion, and skin or eye contact.

• Use gloves, lab coat, and protective eyewear during handling.

• Perform experiments in well-ventilated fume hoods where possible.

• Dispose of contaminated materials according to institutional biosafety protocols.

As a preclinical research compound, observed effects in vitro or in vivo may include altered B-cell proliferation or signaling, but these are experimental endpoints, not clinical side effects. This product is strictly for laboratory use.

Keywords

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Shipping Guarantee

All Orelabrutinib shipments are managed using validated cold-chain logistics to preserve compound integrity. Each order is sealed in moisture-proof, light-resistant packaging with secondary protective wrapping. Real-time temperature monitoring ensures stability during transit. Packages are shipped via international express couriers with full tracking and insurance coverage for global research laboratories.

Trade Assurance

We Orelabrutinib guarantee product authenticity and analytical verification via HPLC, MS, and NMR. Each batch comes with a Certificate of Analysis (CoA) confirming ≥99% purity and identity. Trade assurance includes replacement or refund for deviations from listed specifications, ensuring reliability for reproducible research.

Payment Support

We Orelabrutinib provide flexible, secure payment options for international research clients: PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are encrypted and verified to maintain confidentiality and fund security.

Disclaimer

This Orelabrutinib product is intended for laboratory research use only. It is not for human or veterinary administration. Researchers must follow appropriate safety protocols when handling bioactive compounds. Data generated with Orelabrutinib should not be interpreted as clinical evidence or therapeutic advice.