Description

Product Description

Nilotinib Capsules (CAS 641571-10-0) are a high-purity formulation of a selective BCR-ABL tyrosine kinase inhibitor, widely used in preclinical leukemia research. Nilotinib selectively inhibits BCR-ABL fusion proteins, including mutated forms resistant to first-generation inhibitors, providing a robust tool for mechanistic studies of chronic myeloid leukemia (CML) and related hematologic malignancies.

Mechanism and Molecular Background

The BCR-ABL fusion protein, resulting from the Philadelphia chromosome translocation, drives constitutive tyrosine kinase activity, promoting uncontrolled proliferation and survival of leukemic cells. Nilotinib binds to the ATP-binding site of BCR-ABL, inhibiting its phosphorylation activity, and downstream signaling pathways such as MAPK, PI3K/Akt, and STAT5, ultimately inducing apoptosis and cell cycle arrest in leukemic cells.

The capsule formulation allows reproducible dosing in in vitro and in vivo preclinical models, maintaining high stability and consistent bioavailability. Researchers can model dose-dependent effects on cellular proliferation, apoptosis induction, and signaling modulation using Nilotinib Capsules.

Preclinical Research Applications

Nilotinib Capsules are used for multiple experimental setups:

• Cellular Proliferation Assays: Quantifying growth inhibition in BCR-ABL-positive leukemia cell lines.

• Apoptosis Studies: Assessing caspase activation, Annexin V staining, and DNA fragmentation following BCR-ABL inhibition.

• Drug Resistance Mechanism Studies: Investigating mutations in BCR-ABL that confer resistance to first-generation tyrosine kinase inhibitors.

• Signal Transduction Analysis: Evaluating downstream effects on MAPK/ERK, PI3K/Akt, and STAT pathways.

• Combination Therapy Research: Testing synergistic effects with chemotherapeutic agents or targeted small molecules in preclinical leukemia models.

The high-purity formulation (>99%) ensures that experimental effects are attributable to BCR-ABL inhibition, minimizing variability due to impurities or batch differences.

Quality and Stability

Nilotinib Capsules are manufactured under GMP-compliant conditions, ensuring reproducibility and functional consistency. Each batch is tested using HPLC, MS, and NMR for purity, identity, and structural integrity. Capsules are stable under ambient and refrigerated conditions, allowing flexible storage and experimental use.

The reproducibility and stability make Nilotinib Capsules suitable for:

• In vitro assays requiring precise concentration control.

• Animal studies modeling leukemia progression and response to tyrosine kinase inhibition.

• Mechanistic studies dissecting BCR-ABL-mediated signaling and apoptotic pathways.

Summary

In summary, Nilotinib Capsules (CAS 641571-10-0) provide a high-purity, research-grade BCR-ABL tyrosine kinase inhibitor for preclinical leukemia studies. Their capsule format ensures precise dosing and experimental reproducibility, making them a reliable tool for:

• Mechanistic studies of leukemia cell proliferation and apoptosis

• Investigation of drug resistance and kinase signaling pathways

• Combination therapy research and translational preclinical modeling

Product Specifications

Detailed Description:
Nilotinib Capsules provide a high-purity, research-grade formulation for preclinical studies of BCR-ABL-positive leukemia. The capsules allow reproducible dosing in both in vitro cell culture assays and in vivo animal models, supporting investigations into cellular proliferation, apoptosis, and kinase signaling pathways. GMP production guarantees consistent functional activity, making these capsules suitable for mechanistic studies of drug resistance, combination therapies, and translational research.

Capsule formulation reduces handling variability compared to powders and provides precise delivery of the active compound in leukemia cell lines, xenograft models, or pharmacodynamic assays. Purity verification using HPLC, LC-MS/MS, and NMR ensures experimental reproducibility and supports high-impact mechanistic research.

Mechanism of Action

Nilotinib Capsules (CAS 641571-10-0) are a highly selective BCR-ABL tyrosine kinase inhibitor, designed to target both wild-type and mutant BCR-ABL proteins, including forms resistant to first-generation inhibitors like imatinib. The BCR-ABL fusion protein, resulting from the Philadelphia chromosome translocation (t(9;22)(q34;q11)), exhibits constitutive kinase activity, driving uncontrolled proliferation and survival of leukemic cells. Nilotinib binds to the ATP-binding site of BCR-ABL, preventing substrate phosphorylation and downstream signal propagation.

1. BCR-ABL Kinase Inhibition

Upon administration in preclinical models or in vitro systems, Nilotinib Capsules bind selectively to the ATP-binding pocket of BCR-ABL, effectively inhibiting its kinase activity. This blockade prevents phosphorylation of downstream targets, including CRKL, STAT5, and MAPK/ERK, thereby halting aberrant leukemic cell signaling. Key experimental outcomes include:

• Arrested cell cycle progression in the G1 phase

• Induction of apoptotic pathways via caspase-3 activation

• Suppression of proliferation in BCR-ABL-positive leukemic cells

High-purity Nilotinib Capsules ensure that observed effects are specific to BCR-ABL inhibition, minimizing confounding effects from impurities or batch variability.

2. Downstream Signaling Pathways

Nilotinib influences multiple intracellular pathways central to leukemia pathophysiology:

• MAPK/ERK pathway: Normally promotes cell proliferation; inhibited by Nilotinib, leading to growth suppression.

• PI3K/Akt pathway: Supports cell survival; blockade induces apoptosis.

• STAT5 signaling: Drives transcription of pro-survival genes; inhibited upon Nilotinib treatment, reducing leukemic cell viability.

• CRKL phosphorylation: Reduced CRKL activation serves as a biomarker for Nilotinib efficacy in preclinical assays.

These molecular effects are measurable using western blot, flow cytometry, phospho-specific antibodies, and reporter assays, allowing quantitative assessment of mechanistic outcomes.

3. Induction of Apoptosis

Nilotinib Capsules trigger programmed cell death through both intrinsic and extrinsic apoptotic pathways:

• Mitochondrial depolarization and release of cytochrome c

• Caspase-3 and -9 activation leading to DNA fragmentation

• Modulation of pro- and anti-apoptotic proteins, including Bax, Bcl-2, and survivin

Preclinical studies using Nilotinib Capsules confirm dose-dependent apoptotic responses in BCR-ABL-positive leukemia cell lines, validating the drug’s mechanism and providing insights into resistance mechanisms.

4. Overcoming Drug Resistance

Nilotinib is particularly valuable in resistant leukemia models:

• Inhibits BCR-ABL mutants (e.g., Y253H, E255K, F359V) resistant to first-generation inhibitors

• Reduces clonal expansion of resistant leukemic cells

• Provides a tool for mechanistic studies of secondary resistance and kinase domain mutations

Researchers can use Nilotinib Capsules to evaluate combination therapies and alternative dosing strategies in resistant models, supporting translational preclinical research.

5. Preclinical Applications

Nilotinib Capsules are utilized in multiple research contexts:

• In vitro proliferation assays in leukemia cell lines

• Apoptosis and cytotoxicity studies for mechanistic elucidation

• Signal transduction analysis of MAPK/ERK, PI3K/Akt, and STAT5 pathways

• Combination therapy research: synergistic effects with other kinase inhibitors, chemotherapeutics, or targeted therapies

• Biomarker identification for BCR-ABL activity and response prediction

The capsules provide consistent dosing, enabling reproducible results across experimental models, including both cellular and animal studies.

6. Summary

In summary, Nilotinib Capsules (CAS 641571-10-0) act as a potent and selective BCR-ABL tyrosine kinase inhibitor, effectively halting leukemic cell proliferation, inducing apoptosis, and modulating key intracellular signaling pathways. Their high-purity, research-grade formulation makes them a reliable tool for mechanistic leukemia studies, drug resistance investigations, and combination therapy research, supporting both in vitro and in vivo preclinical models.

Side Effects

Nilotinib Capsules (CAS 641571-10-0), while designed exclusively for preclinical and laboratory research, exhibit measurable cellular and molecular effects that are critical for researchers to consider when designing experiments. These effects are consistent with its mechanism as a BCR-ABL tyrosine kinase inhibitor and are valuable for mechanistic studies but require careful experimental design to avoid confounding outcomes.

1. Cellular Effects

Exposure to Nilotinib Capsules in cell culture systems leads to:

• Inhibition of proliferation: BCR-ABL-positive leukemia cells show a dose-dependent reduction in growth.

• Induction of apoptosis: Observed via caspase activation, Annexin V staining, and DNA fragmentation.

• Altered cell cycle dynamics: Arrest in the G1 phase due to inhibited kinase signaling.

While these effects are intended for mechanistic studies, excessive concentrations can result in non-specific cytotoxicity, affecting control cell populations.

2. Molecular and Signaling Effects

At the molecular level, Nilotinib blocks BCR-ABL-mediated phosphorylation, resulting in:

• Downregulation of CRKL phosphorylation, a direct marker of BCR-ABL activity.

• Inhibition of MAPK/ERK and PI3K/Akt pathways, reducing survival signaling.

• Suppression of STAT5 activation, decreasing transcription of anti-apoptotic genes.

• Modulation of apoptotic proteins, including Bax, Bcl-2, and survivin, leading to programmed cell death.

These effects are experimentally desirable but should be quantified carefully to distinguish between specific BCR-ABL inhibition and off-target kinase effects.

3. Laboratory Handling Considerations

Although formulated in capsules for precise dosing, Nilotinib remains a bioactive small molecule. Proper laboratory handling includes:

• PPE: Gloves, lab coat, and eye protection.

• Use of fume hoods for powder transfer or capsule dissolution.

• Avoiding repeated freeze-thaw cycles to maintain activity.

• Proper disposal of residual material to prevent environmental contamination.

Following these precautions ensures both safety and reproducibility of experimental results.

4. Off-Target Effects

High concentrations of Nilotinib Capsules may lead to off-target kinase inhibition, including c-KIT, PDGFR, and other tyrosine kinases. Researchers should:

• Conduct dose-response studies to identify optimal experimental concentrations.

• Include appropriate negative controls and isotype controls.

• Validate findings using complementary techniques such as siRNA knockdown or CRISPR-mediated gene editing.

These steps minimize confounding results in mechanistic and translational studies.

5. Summary

In preclinical research, Nilotinib Capsules (CAS 641571-10-0) effectively inhibit BCR-ABL activity, modulate downstream signaling, induce apoptosis, and halt proliferation in leukemia models. Awareness of cellular and molecular effects, proper laboratory handling, and careful experimental design are essential to ensure reproducible results. These features make Nilotinib Capsules an indispensable tool for mechanistic leukemia research, drug resistance studies, and preclinical therapy evaluation.

Keywords

Nilotinib Capsules, CAS 641571-10-0, BCR-ABL tyrosine kinase inhibitor, chronic myeloid leukemia research, leukemia cell line study, drug resistance research, preclinical leukemia models, kinase signaling modulation, high-purity small molecule, mechanistic leukemia study, translational cancer research, combination therapy evaluation, factory small-molecule supplier, China chemical manufacturer, bulk production research-grade, high-purity research reagent.

Shipping Guarantee

Nilotinib Capsules (CAS 641571-10-0) are shipped under strict temperature-controlled conditions to preserve chemical stability and activity. Packaging is insulated, tamper-evident, and includes real-time tracking and insurance coverage. International delivery options, express shipping, and cold-chain logistics ensure that capsules arrive at research laboratories in optimal condition for preclinical and mechanistic studies.

Trade Assurance

All batches of Nilotinib Capsules are produced under GMP-compliant standards with purity ≥99% verified by HPLC, LC-MS/MS, and NMR. Certificates of Analysis (CoA) accompany each lot. Bulk production, OEM, and customized concentrations are available. The manufacturer provides reliable replacement or return policies, ensuring consistent experimental reproducibility.

Payment Support

Payment options include PayPal, major credit cards, T/T, USDT, Bitcoin, and Ethereum. Transactions are fully encrypted, enabling secure and global procurement of high-purity Nilotinib Capsules for preclinical leukemia research and mechanistic studies.

Disclaimer

Nilotinib Capsules (CAS 641571-10-0) are intended exclusively for laboratory and preclinical research use. They are not for human or veterinary administration. Researchers must follow biosafety protocols, use appropriate PPE, and handle capsules according to GLP standards. Improper use may alter experimental outcomes. All content is provided for scientific research purposes only.

References

1. PubChem – Nilotinib
   Provides detailed molecular structure, physicochemical properties, and bioactivity data for Nilotinib, supporting preclinical leukemia research.

2. ChEMBL – Nilotinib
   Contains bioactivity profiles, molecular target interactions, and experimental assay data suitable for mechanistic studies of BCR-ABL inhibition.

3. DrugBank – Nilotinib
   Provides pharmacological information, mechanism of action insights, and preclinical applications of Nilotinib Capsules.

4. PubMed – Nilotinib Research Articles
   Access peer-reviewed publications detailing BCR-ABL inhibition, leukemia cell proliferation, apoptosis, and resistance mechanisms.

5. IUPHAR/BPS – Tyrosine Kinase Targets
   Curated data on kinase targets, signaling pathways, and molecular interactions relevant to Nilotinib Capsules research.

6. Additional Resources

• ACS Pharmacology & Translational Science.

• Sigma-Aldrich Technical Datasheets on Nilotinib.

• ResearchGate Experimental Studies on BCR-ABL Inhibitors.

These references provide authoritative, peer-reviewed information for laboratories using Nilotinib Capsules (CAS 641571-10-0) in mechanistic, preclinical, and translational leukemia research. They support molecular data, functional assay protocols, and experimental design for reproducible and high-impact studies.