Navitoclax-Piperazine: Properties, Handling & Research Use Guide
Navitoclax-Piperazine: Properties, Handling & Research Use Guide
Navitoclax-piperazine is a piperazine-containing analogue of Navitoclax designed to retain potent BCL-2 family protein inhibition while offering researchers an alternative chemical scaffold for apoptosis and senolytic research applications.
- Product Name
- Navitoclax-piperazine
- SKU
- N649050
- Cross-Reference
- MCE: HY-44432
- Primary Target Class
- BCL-2 family anti-apoptotic proteins (BH3 mimetic)
- Key Research Application
- Apoptosis induction, senolytic studies, cancer biology
- Recommended Storage
- -20 °C, protected from light and moisture (general small-molecule guideline; verify CoA)
Compound Overview and Mechanism of Action
Navitoclax-piperazine (Aladdin SKU: N649050; cross-reference MCE HY-44432) is a synthetic small molecule belonging to the BH3-mimetic class of compounds. BH3 mimetics are designed to occupy the hydrophobic groove of anti-apoptotic BCL-2 family proteins—including BCL-2, BCL-XL, and BCL-W—thereby displacing pro-apoptotic BH3-only proteins and releasing the apoptotic cascade.
The piperazine modification in the core scaffold relative to the parent compound Navitoclax is intended to modulate physicochemical properties such as aqueous solubility, pKa, and membrane permeability. Such structural variations are a common medicinal-chemistry strategy to optimize pharmacokinetic behavior while preserving target engagement. Researchers should consult the product Certificate of Analysis (CoA) and primary literature for confirmed binding affinities and selectivity data specific to this analogue.
Research Applications
Apoptosis Research: As a BH3 mimetic, Navitoclax-piperazine is suitable for in vitro studies aimed at understanding the mitochondrial (intrinsic) apoptotic pathway. It can be used to probe the dependence of cancer cell lines on specific anti-apoptotic BCL-2 family members for survival.
Senolytic Studies: Navitoclax and its analogues have been investigated as senolytics—agents that selectively eliminate senescent cells. Navitoclax-piperazine may be employed in cellular senescence models to evaluate its capacity to clear senescent cells, contributing to research on aging and age-related pathologies.
Combination Studies: BH3 mimetics are frequently evaluated in combination with other targeted agents (e.g., kinase inhibitors, DNA-damaging agents) to assess synergistic or additive anti-tumor effects. Navitoclax-piperazine may serve as a tool compound in such mechanistic combination screens.
Note: This product is for research use only (RUO). It is not approved for diagnostic or therapeutic use in humans or animals.
Handling, Storage and Solution Preparation
Storage: Store at -20 °C in a tightly sealed container, protected from light and moisture. Allow the vial to equilibrate to room temperature before opening to prevent condensation. Always verify conditions stated on the product CoA, as lot-specific instructions take precedence.
Solubility and Vehicle Selection: BH3-mimetic small molecules with piperazine moieties typically exhibit enhanced aqueous solubility compared to their parent structures. DMSO is a common primary solvent for preparing concentrated stock solutions (e.g., 10–50 mM). For cell-based assays, dilute DMSO stocks into aqueous media such that the final DMSO concentration does not exceed 0.1–0.5% (v/v) to avoid cytotoxic artefacts. Confirm solubility experimentally and consult the CoA for supplier-verified solubility data.
Stock Preparation: Prepare single-use aliquots to minimize freeze-thaw cycles. Label each aliquot with compound identity, concentration, solvent, date of preparation, and operator initials. Store aliquots at -20 °C or as specified on the CoA.
Safety: Handle all cytotoxic or biologically active research compounds in a well-ventilated fume hood or biosafety cabinet. Wear appropriate PPE (gloves, lab coat, eye protection). Consult the Safety Data Sheet (SDS) before use.
Quality, Purity and Verification
Research-grade compounds from Aladdin Scientific undergo quality control to ensure identity and purity. For Navitoclax-piperazine (N649050), researchers are advised to:
- Review the Certificate of Analysis (CoA) for purity (typically assessed by HPLC), identity confirmation (e.g., MS, NMR), and lot-specific data before initiating experiments.
- Perform an independent activity assay (e.g., cell viability assay in a BCL-2-dependent cell line) as a functional verification step when establishing the compound in a new laboratory workflow.
- Use appropriate positive and negative controls in all assays to confirm compound activity and exclude non-specific effects.
If you require a specific purity grade or additional characterization data (e.g., endotoxin testing), contact Aladdin Scientific's technical support team.
Ordering and Technical Support
Navitoclax-piperazine is available from Aladdin Scientific under SKU N649050. To place an order or request a quotation, contact your regional Aladdin Scientific representative or visit the Aladdin Scientific website.
For technical enquiries regarding solubility, assay compatibility, or custom synthesis requirements, Aladdin Scientific's scientific support team is available to assist. Please have the product SKU and your experimental context ready when contacting support to ensure the most relevant guidance.
Cross-reference: This compound corresponds to MCE catalogue number HY-44432, which may assist researchers in locating published experimental protocols referencing that identifier.
Frequently asked questions
What is Navitoclax-piperazine and how does it differ from Navitoclax?
Navitoclax-piperazine is a structural analogue of Navitoclax in which a piperazine moiety has been incorporated into the chemical scaffold. Like Navitoclax, it belongs to the BH3-mimetic class and targets anti-apoptotic BCL-2 family proteins. The piperazine modification is a medicinal-chemistry strategy commonly employed to alter solubility, pKa, or pharmacokinetic properties relative to the parent compound. Researchers should consult primary literature and the CoA for confirmed experimental data on this analogue.
What solvent should I use to dissolve Navitoclax-piperazine for cell-based assays?
DMSO is the most commonly used solvent for preparing concentrated stock solutions of BH3-mimetic compounds. Prepare a stock at 10–50 mM in DMSO, then dilute into cell culture medium to achieve the desired working concentration, ensuring the final DMSO content does not exceed 0.1–0.5% (v/v). Always verify solubility on the product CoA and include a vehicle-only control in your assay design.
Is Navitoclax-piperazine suitable for in vivo studies?
Navitoclax-piperazine (N649050) is supplied as a research-use-only reagent and has not been evaluated or approved for in vivo therapeutic use. Researchers intending to use BH3-mimetic analogues in animal studies should conduct thorough literature review, formulation development, and appropriate institutional ethics approval. Consult Aladdin Scientific's technical support for guidance on suitable formulation vehicles.
What quality control data is available for N649050?
Each lot of Navitoclax-piperazine (N649050) is accompanied by a Certificate of Analysis (CoA) that typically includes purity data (HPLC), structural identity confirmation (MS and/or NMR), and lot-specific results. Download the CoA from the Aladdin Scientific product page or request it from your sales representative. If additional characterization such as endotoxin testing is required, contact technical support.
References
- Tse C, et al. ABT-263: A potent and orally bioavailable Bcl-2 family inhibitor. Cancer Research, 2008. [Navitoclax parent compound reference — verify applicability to piperazine analogue]
- Zhu Y, et al. New agents that target senescent cells: the flavone, navitoclax, and their combinations. Aging (Albany NY), 2017. [Senolytic application of Navitoclax class — verify relevance to piperazine analogue]
- MCE Product Reference: HY-44432, Navitoclax-piperazine. MedChemExpress. [Cross-reference catalogue entry — consult for supplier-provided physicochemical data]
Products are supplied for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
危险品化学品经营许可证(带存储)