GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.
This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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Application Protocols
Validated, item-specific application protocols are not provided in the product data for this SKU.
Tested applications: Not specified for this item; refer to CoA/Spec Sheet.
Recommended working concentrations/dilutions: Not specified for this item; refer to CoA/Spec Sheet.
Positive controls/assay references: Not specified for this item; refer to CoA/Spec Sheet.
General suggestion:
When developing new assays, include a vehicle control matching the final DMSO percentage and a titration series (e.g., half-log dilutions) spanning anticipated potency ranges, with appropriate replicate numbers and orthogonal readouts. These are general best practices and not validated for this specific item.
Biological Roles
Context (literature/general):
Vepafestinib is described in the literature as a small-molecule tyrosine kinase inhibitor with selectivity for the RET kinase family. Such inhibitors act by occupying the ATP-binding site of the kinase domain, thereby modulating phosphorylation signaling cascades.
Pathway considerations (general):
RET signaling influences downstream pathways such as MAPK/ERK and PI3K/AKT. Chemical inhibition can be used to probe pathway dependencies, feedback regulation, and adaptive resistance mechanisms in engineered cell models.
Research uses enabled by such probes:
Define structure–activity relationships (SAR) around the RET active site via biochemical potency and cellular target engagement assays.
Study resistance mechanisms (e.g., gatekeeper or solvent-front mutations) by comparing inhibition profiles across RET variants.
Evaluate CNS-penetration–relevant physicochemical parameters in preclinical models if blood–brain barrier transport is a research objective; refrain from any clinical claims.
Important caveats:
Do not infer therapeutic efficacy or safety from in vitro results. Use appropriate positive/negative controls and orthogonal assay readouts (biochemical plus cellular). Confirm on-target effects with genetic tools (siRNA/CRISPR) where possible.
Item-specific note:
This SKU is provided for research use only. Definitive biological activity, potency, and selectivity values for the lot are Not specified for this item; refer to CoA/Spec Sheet and primary literature for quantitative data.
Buffer Applications
This compound is not a buffering agent and is not typically used to prepare laboratory buffers.
Practical note: For biological assays, vepafestinib is commonly dosed from DMSO stocks into pre-made buffers (e.g., HEPES- or PBS-based), maintaining a consistent and low final DMSO percentage across all wells/samples.
If solubility issues arise upon dilution, consider adding a non-ionic surfactant (e.g., 0.01–0.05% Tween-80) or using protein-containing media to enhance apparent solubility. Validate that additives do not interfere with the assay readout.
Green Alternatives
This product is a discrete bioactive small molecule, not a process solvent or reagent used in bulk transformations. “Green alternatives” therefore relate to handling and formulation practices rather than substituting the compound itself.
Use minimal DMSO percentages in biological assays (e.g., ≤0.1–0.5% v/v) to reduce solvent burden on cells and wastewater.
Prefer ethanol or water-miscible greener co-solvents where compatible (EtOH over DMF/NMP). Validate solubility and assay performance.
Apply microscale workflows (96/384-well plates, automated liquid handling) to minimize compound and solvent consumption.
Opt for sealed, low-dead-volume vials and cold-plate dispensers to cut evaporative losses and repeat thaw/freeze.
For purification/analysis, adopt greener chromatographic conditions (e.g., H2O/EtOH or H2O/ACN with formic acid) when feasible.
Illustrative comparison (general):
DMSO vs DMF/NMP for stock prep: DMSO is broadly preferred due to lower toxicity and better biodegradability profile relative to DMF/NMP. If DMSO is unsuitable, ethanol/propylene carbonate mixtures may be explored case-by-case.
Waste considerations:
Segregate DMSO- and acetonitrile-containing waste. Avoid halogenated solvents unless required analytically. Follow institutional green-chemistry and waste-minimization policies.
Pharmaceutical Uses
No excipient role or pharmacopeial monograph is provided for this item. This product is supplied strictly for research use.
Research/manufacturing context (general):
Reference standard: May serve as a reference material for analytical method development (e.g., identity/purity assays by LC–MS) in discovery settings.
Preformulation research: Solubility screening, salt/solid-form exploration, and compatibility studies with common excipients can be performed to understand physicochemical behavior, without implying clinical application.
Stability studies: Forced-degradation and photostability experiments can map degradation pathways to guide storage/formulation of kinase inhibitors broadly.
Regulatory note:
Not for human or veterinary use. No claims of safety, efficacy, or GMP status. Any scaling or translational use requires independent qualification to applicable standards.
Physical Properties
Item-specific physical constants are not provided in the product data for this SKU. Consult the CoA/SDS for definitive values.
Appearance: Not specified for this item; refer to CoA/Spec Sheet.
Melting point: Not specified for this item; refer to CoA/Spec Sheet.
Boiling point: Not applicable (decomposes) for most complex drug-like solids; specific value Not specified for this item; refer to CoA/Spec Sheet.
Density: Not specified for this item; refer to CoA/Spec Sheet.
LogP/logD: Not specified for this item; refer to CoA/Spec Sheet.
pKa(s): Not specified for this item; refer to CoA/Spec Sheet.
UV-Vis: Not specified for this item; refer to CoA/Spec Sheet.
Solubility profile (general/literature guidance for kinase inhibitors):
Organic: often soluble in DMSO, DMF, or NMP at 10–50 mM; partial solubility in ethanol/MeOH; exact solubility for this item is Not specified—verify experimentally.
Aqueous: frequently low intrinsic solubility at neutral pH; may require co-solvent or pH adjustment. For bioassays, DMSO stock followed by aqueous dilution with surfactant (0.01–0.1% Tween-80) is commonly used in literature.
Practical tips (general):
Prepare a small trial stock (e.g., 10 mM in anhydrous DMSO), vortex/sonicate, and visually inspect for clarity/precipitation after dilution into assay buffer. Filter if needed using low-binding PTFE/nylon filters. Record final %DMSO in assays to maintain consistency across controls.
Quality and Grades
Supplied grade: Moligand™ (as listed in product data).
What Moligand™ typically implies (general guidance):
Research screening/ligand grade intended for discovery biology and medicinal chemistry workflows (e.g., target validation, assay development, probe studies).
Emphasis on identity confirmation and suitability for biochemical/cellular assays. Typical library-grade practices include NMR/LC–MS confirmation, and purity optimized for screening; however, specific purity and analytical thresholds for this SKU are Not specified for this item; refer to CoA/Spec Sheet.
Implications for use:
Suitable for in vitro enzyme assays, cell-based pathway interrogation, and as a reference/positive control in HTS or targeted profiling.
For quantitative bioanalytical work (calibration standards) or in vivo studies, verify lot-specific purity, residual solvents, counter-ions, and water content directly from the CoA. If tighter specifications (e.g., metal content, residual reagents) are needed, consider performing additional in-house qualification.
Stabilizers/additives:
Not specified for this item; refer to CoA/Spec Sheet. If stabilizers are present (e.g., acid salts, antioxidants), account for them in molecular weight corrections for stock solutions.
Documentation:
Request the lot-specific Certificate of Analysis (CoA) for identity confirmation, purity, analytical chromatograms, and recommended handling/storage.
Reaction and Applications
This product is intended as a bioactive small-molecule research tool rather than a synthetic reagent. Accordingly, its primary “applications” are in chemical biology and assay development.
Research/assay applications (literature/general):
Kinase pathway studies: Use as a small-molecule probe to interrogate signaling cascades downstream of its reported target class (RET tyrosine kinase per literature), enabling target validation and mechanistic studies in cell lines engineered for pathway readouts (e.g., phosphorylation biomarkers).
Biochemical profiling: Determine potency and selectivity using recombinant kinase panels; characterize binding kinetics (Kd, kinact/Ki if covalent—not typically reported for vepafestinib) by SPR, ITC, or enzymatic inhibition assays.
Cellular assays: Assess inhibition of pathway activation with Western blot or ELISA for phospho-substrates; evaluate transcriptomic responses to target blockade.
ADME/PK research: Solubility, microsomal stability, permeability (PAMPA/MDCK), and protein binding to support probe deployment; avoid clinical extrapolation.
Analytical applications:
Use as a reference standard for chromatographic method development (LC–UV/LC–MS) in complex matrices relevant to discovery biology (cell lysates, microsomes).
Notes:
No reaction chemistry applications are typical for this final API-like small molecule. If chemical modification is desired (e.g., probe derivatization), de novo synthesis or late-stage functionalization strategies should be considered by medicinal chemists, using vepafestinib only as a comparative control.
Reaction Conditions
This product is not intended for use as a reagent in synthetic transformations. Typical “reaction conditions” therefore focus on solution preparation and assay dosing protocols (general guidance):
Stock solutions:
Solvent: anhydrous DMSO (preferred). Alternative: DMF or ethanol if compatible with the assay.
Concentration: commonly 10–50 mM; confirm solubility empirically for this item (Not specified for this item; refer to CoA/Spec Sheet).
Aids: brief sonication and mild warming (≤40°C) can assist dissolution.
Assay dosing:
Dilute DMSO stocks into pre-equilibrated assay buffer or media with vigorous mixing to avoid local supersaturation. Maintain consistent final DMSO across wells/samples (e.g., 0.1–0.5% v/v).
Incubation times and temperatures depend on the biological assay (enzyme vs cell-based). Typical enzyme inhibition assays run at 25–37°C for 10–60 minutes; cell assays 1–24 hours. Optimize per protocol.
Stability checks:
Monitor by LC–MS/UPLC for degradation over time in stock and working solutions. Protect from extended light exposure if photosensitive (verify via SDS/CoA). Conduct freeze–thaw cycling studies if aliquoting.
Note: For any chemical transformation involving this molecule (e.g., analytical derivatization), conditions must be developed de novo; no standard synthetic reaction conditions are provided for this item.
Safety and Handling
Hazard classification for this specific item is not provided in the product data. Always consult the SDS for authoritative information.
GHS classification, pictograms, signal word, H-statements: Not specified for this item; refer to SDS.
General laboratory safety guidance (for small-molecule kinase inhibitors):
PPE: Use lab coat, safety glasses, and appropriate chemical-resistant gloves (nitrile). Avoid skin contact, inhalation of dust/aerosols, and ingestion.
Handling: Work in a fume hood or ventilated enclosure when weighing powders or preparing solutions. Minimize dust generation. Use closed containers and secondary containment for transport within the lab.
Incompatibilities: Avoid strong oxidizers and strong acids/bases unless part of a controlled procedure. Protect from prolonged light exposure if compound is photosensitive (verify on SDS/CoA).
First aid (overview; defer to SDS):
Inhalation: Move to fresh air; seek medical attention if symptoms persist.
Skin/eye contact: Rinse with water for at least 15 minutes; remove contaminated clothing; seek medical advice if irritation occurs.
Ingestion: Rinse mouth; do not induce vomiting; seek medical attention.
Spill/leak: Avoid dust; collect with damp disposable towels or HEPA vacuum; place waste in a sealed container for hazardous disposal.
Waste: Dispose of in accordance with institutional and local regulations; avoid drain disposal.
Special notes:
Biologically active research compounds should be handled with care at milligram-to-gram scale to prevent unintended exposure. Implement good hygiene and clean surfaces after use.
Solvent Selection
Since vepafestinib is a complex, largely hydrophobic small molecule, organic polar aprotic solvents are typically preferred for stock solution preparation (general guidance).
Polarity/miscibility (general):
DMSO: broad solvating power for kinase inhibitors; miscible with water—most common for assay stocks.
DMF or NMP: strong solvents; use when DMSO solubility is insufficient; consider cytotoxicity when dosing cells.
Ethanol/MeOH: moderate solubility; useful for analytical sample prep; mind volatility.
Aqueous buffers: often limited solubility without co-solvent or pH modification.
Selection guidance:
Primary choice: anhydrous DMSO for 10–50 mM stocks (verify solubility empirically for this item).
For biophysical assays sensitive to DMSO: explore DMF or MeOH at low final percentages, or prepare mixed-solvent systems (e.g., DMSO:buffer 1:9, with gentle heating and sonication).
LC–MS sample prep: ACN/H2O with 0.1% formic acid often works after a DMSO pre-dissolution step.
Comparison (general considerations):
DMSO: best solubility; low volatility; potential biological effects above ~0.5–1% v/v in cell assays.
DMF/NMP: strong solvation; higher cytotoxicity risk; less desirable for live-cell work.
Warm (30–40°C) and sonicate resistant solids briefly. Avoid prolonged heating. Filter stocks if particulates persist. Record and match final solvent percentages across controls and test wells.
Shipped in: Not specified for this item; refer to CoA/Spec Sheet.
Reconstitution/solution preparation:
Reconstitution solvent: Not specified for this item; refer to CoA/Spec Sheet.
General guidance (literature/practice): Dissolve in anhydrous DMSO to prepare a concentrated stock (e.g., 10–50 mM, as solubility permits). Sonicate and gently warm (≤40°C) if needed. Filter through a low-binding 0.2 µm PTFE filter if particulates persist.
Aliquoting: Dispense single-use aliquots in inert vials to avoid repeated freeze–thaw. Clearly label concentration, solvent, and date.
Stability considerations:
Solid state: Store tightly closed, protected from moisture and prolonged light. While room-temperature storage is indicated, cooler, desiccated storage can further enhance longevity for many kinase inhibitors; follow CoA/SDS guidance.
Solutions: DMSO stocks are typically stable for weeks at −20°C to −80°C (general practice). Verify stability of this specific item by periodic LC–MS/UPLC.
Handling notes:
Equilibrate cold aliquots to room temperature before opening to prevent moisture condensation. Record %DMSO in working solutions and maintain consistency across experiments.
Research use note: For research use only.
Structure and Identity
Overview: Vepafestinib is a small-molecule kinase inhibitor supplied as a screening/ligand compound (Moligand grade) for research use.
Product identifiers (item-specific):
SKU: V614730
Product name: vepafestinib
CAS: 2129515-96-2
PubChem CID: 134164132
InChIKey: Not specified for this item; refer to CoA/Spec Sheet. (Product data lists an incomplete key.)
SMILES: Not specified for this item; refer to CoA/Spec Sheet.
Composition:
Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
Structural features (literature/general):
Vepafestinib is reported in the literature as a heteroaromatic, nitrogen-rich, ATP-competitive tyrosine kinase inhibitor scaffold, typically incorporating multiple fused/aromatic rings and heteroatoms (N, O) that support hinge-binding and solvent-front interactions common to kinase inhibitors.
2D-structure description (literature-level): a polycyclic heteroaromatic core bearing hydrogen-bond donor/acceptor motifs (e.g., amide/urea-like linkers) and substituents tuned for kinase selectivity and CNS/permeability in some reports. Stereochemistry is generally not a defining feature (commonly achiral), but confirm on the CoA.
Notes:
For definitive structural strings (SMILES/InChI), exact molecular formula, and MW applicable to this supplied lot, consult the product CoA or Spec Sheet. The above “literature/general” comments are provided for orientation only.
Synthetic Utility
Vepafestinib is a complex, drug-like final compound and is not generally employed as a synthetic building block.
Medicinal chemistry context (general):
Serves as a benchmark/positive control when designing and testing analogs that target the same kinase binding site.
May guide retrosynthetic planning for related scaffolds: common motifs in kinase inhibitors include hinge-binding heteroaromatics, amide/urea linkers, and solubilizing substituents. However, late-stage diversification of the intact molecule is limited due to functional group density and potential liability to harsh conditions.
Analytical/synthetic support uses:
Calibration standard for LC–MS during synthesis of analog series.
Spike-and-recovery experiments in biological matrices to qualify extraction and quantitation protocols.
If derivatization is desired:
Consider de novo synthesis routes to install reporter handles (alkynes/azides) or photoreactive groups prior to the final coupling steps, rather than modifying vepafestinib directly. Photolabels or biotin handles can be integrated into analogs for chemoproteomics, with vepafestinib retained as the non-modified control.
Target Specificity
Only target-related details explicitly provided in the product data may be listed here.
Target/class: Not specified for this item; refer to CoA/Spec Sheet.
Species reactivity/assay context: Not specified for this item; refer to CoA/Spec Sheet.
Selectivity panel data: Not specified for this item; refer to CoA/Spec Sheet.
Note: Consult primary literature and the lot-specific documentation for quantitative potency and selectivity information, if available.
Need help choosing the grade?
Our grade selection guide covers purity, stabilizer status, and application suitability for all variants in our catalog.
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