GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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Information
Masitinib is a novel inhibitor forKit (c-Kit)andPDGFRα/βwithIC50of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. In vitro
Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, Masitinib demonstrates weak inhibition of Abl and c-Fms. Masitinib more strongly inhibits degranulation, cytokine production, and bone marrow mast cell migration than imatinib. In Ba/F3 cells expressing human wild-type Kit, Masitinib inhibits SCF (stem cell factor)-induced cell proliferation with an IC50 of 150 nM, while the IC50 for inhibition of IL-3-stimulated proliferation is at approximately >10 µM. In Ba/F3 cells expressing PDGFRα, Masitinib inhibits PDGF-BB-stimulated proliferation and PDGFRα tyrosine phosphorylation with IC50 of 300 nM. Masitinib also causes inhibition of SCF-stimulated tyrosine phosphorylation of human Kit in mastocytoma cell-lines and BMMC. Masitinib inhibits Kit gain-of-function mutants, including V559D mutant and Δ27 mouse mutant with IC50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC50 of 10 and 30 nM, respectively. Masitinib inhibits cell growth and PDGFR phosphorylation in two novel ISS cell lines, which suggest that Masitinib displays activity against both primary and metastatic ISS cell line and may aid in the clinical management of ISS.
In vivo
Masitinib inhibits tumour growth and increases the median survival time in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity or genotoxicity. Masitinib (12.5 mg/kg/d PO) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. The combination of masitinib/gemcitabine shows synergy in vitro on proliferation of gemcitabine-refractory cell lines Mia Paca2 and Panc1, and to a lesser extent on Mia Paca-2 pancreatic tumours in Nog璖CID mice. Cell Data
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Application Protocols
No item-specific, validated application protocols are provided in the Product Data for this SKU.
General research-use guidance:
Biochemical kinase assay:
Prepare a DMSO stock, perform a 10-point half-log dilution series, and incubate with enzyme (with Mg2+/ATP as required) for 10–30 min before initiating reaction.
Readouts: ADP-coupled assays, TR-FRET, fluorescence polarization, or radiometric formats; fit dose–response to obtain IC50.
Cell-based assay:
Dilute compound into complete media ensuring final DMSO ≤0.5% v/v. Include vehicle controls and, where appropriate, orthogonal readouts (e.g., p-KIT Western blot, phospho-RTK arrays).
Target engagement/biophysics:
Use thermal shift (DSF/CETSA) or BRET target engagement assays to confirm on-target binding in the chosen system.
Adapt these templates to your instrumentation and SOPs; validate performance with internal controls.
Biological Roles
General, literature-level information for research use (no clinical claims):
Masitinib (AB1010) is widely cited as a small-molecule tyrosine kinase inhibitor used to interrogate signaling pathways in biochemical and cellular systems. Literature reports describe activity against class III receptor tyrosine kinases (e.g., KIT, PDGFR) and certain Src-family kinases, supporting its use as a probe compound for oncogenic and mast-cell signaling research.
Mechanistic context:
Functions as an ATP-competitive inhibitor occupying the kinase catalytic cleft, thereby modulating phosphorylation cascades downstream of the targeted kinases.
Selectivity profiles in publications frequently highlight potency on mutant and wild-type KIT, making it a reference for mast cell biology studies.
Research utility:
Tool for mapping phosphoproteomic changes upon kinase blockade.
Benchmark in structure–activity relationship (SAR) comparisons within phenyl/heteroaryl kinase inhibitor chemotypes.
Control compound in target engagement assays (thermal shift/DSF, CETSA, BRET) to validate assay responsiveness.
Notes:
Potency values (IC50/Ki), specific target panels, and cellular phenotypes vary by study design and test conditions; consult primary literature and generate matrix-specific dose–response curves in your laboratory.
Buffer Applications
This compound is a bioactive small molecule rather than a buffering agent. It is not used to establish or maintain pH.
Practical notes for assay buffers (general):
Prepare working solutions by diluting DMSO stocks into a compatible assay buffer (e.g., HEPES or Tris for biochemical assays; culture media for cell assays), maintaining final DMSO typically ≤0.5–1% v/v.
Include detergent (e.g., 0.01% Tween-20) in biochemical buffers if colloidal aggregation is suspected.
For kinase assays, buffers commonly include Mg2+ and ATP; ensure inhibitor pre-incubation (e.g., 10–30 min) to reach equilibrium before initiating reactions.
No item-specific buffer recipes are provided; optimize for your assay format.
Green Alternatives
While Masitinib itself is a target molecule rather than a solvent or reagent, greener practices can be applied to its handling, formulation, and analysis.
Solvent considerations (general):
Prefer water-miscible systems with minimal DMSO content in final assays (≤0.5% v/v) to reduce solvent burden.
For preparative work, consider EtOH/H2O or MeOH/H2O co-solvent systems over DMF/NMP where feasible.
For LC separations, ACN often affords lower backpressure and is easier to recover than MeOH in some labs; evaluate solvent recycling where infrastructure exists.
Process and waste minimization:
Use miniaturized assays (384/1536-well) to decrease compound and solvent consumption.
Implement automated low-volume dispensing and sealed plates to minimize volatilization and exposure.
Consolidate analytical runs and adopt UPLC to reduce mobile-phase use.
Comparison (general guidance):
DMSO vs EtOH co-solvent: DMSO maximizes solubility but raises dermal absorption concerns; EtOH mixtures may be greener but can limit achievable concentration.
DMF/NMP (problematic) vs PEG400/aqueous surfactants: PEG systems can enable aqueous formulations but may complicate analytics; choose based on end-use and disposal capabilities.
All substitutions should be validated for assay performance and compound stability.
Pharmaceutical Uses
Research-use context only (no clinical or therapeutic claims):
Can serve as an analytical reference material for method development and validation (e.g., LC-UV/LC-MS calibration, specificity, linearity) in laboratories studying tyrosine kinase inhibitors.
Useful as a system suitability standard for chromatographic methods evaluating basic, moderately lipophilic small molecules.
Employed in formulation research to explore solubilization strategies for basic kinase inhibitors (e.g., DMSO concentrates, cosolvent systems, pH adjustment, salt screening) with subsequent non-clinical in vitro testing.
Applicable in stability-indicating method development, including stress studies (acid/base, oxidative, thermal, photolytic) to map degradation pathways of related chemotypes.
Item-specific pharmacopeial status, compendial monographs, or impurity standards: Not specified for this item; refer to CoA/Spec Sheet and current pharmacopeias if needed.
Physical Properties
Item-specific physical specifications are not provided in the Product Data for this listing. Please consult the CoA/Spec Sheet for values used in release testing.
Appearance (item-specific): Not specified for this item; refer to CoA/Spec Sheet.
Melting point, boiling point, density, refractive index (item-specific): Not specified for this item; refer to CoA/Spec Sheet.
Solubility guidance (general/literature-level for kinase inhibitors of this class; not item-specific):
Frequently soluble in DMSO at stock concentrations (e.g., 10–50 mM typical for screening), miscible with DMF and other polar aprotic solvents.
Often sparingly soluble in aqueous buffers at neutral pH unless co-solvents or salts are employed. Aqueous solubility can increase upon salt formation (e.g., HCl, mesylate), if applicable to the supplied form.
Ethanol/MeOH can aid co-solubilization, but DMSO is the most common vehicle for HTS and biochemical assays.
LogP, pKa (literature/computational expectations for a basic, multi-aryl kinase inhibitor; not item-specific):
Presence of a tertiary amine suggests at least one basic pKa in the 7–10 range (literature-class trend), enabling protonation in aqueous media.
Overall lipophilicity is typically moderate-to-high for target engagement within kinase ATP sites.
Always verify actual solubility and physical constants for your lot with the CoA and perform a small-scale solubility screen prior to critical experiments.
Quality and Grades
Supplied grade: Moligand™ (item-specific). This denotes a research-use small-molecule/ligand quality intended for discovery chemistry, target validation, and screening workflows.
What Moligand™ typically implies (general guidance; confirm with CoA):
Emphasis on chemical identity and purity appropriate for medicinal chemistry and assay deployment. Impurity profile and residual solvents are controlled per internal specifications.
Packaged to support assay-ready handling (e.g., compatibility with DMSO dissolution and plate-based dispensing).
Not manufactured to cGMP; not for human or veterinary use, diagnostic use, or as a drug substance. See “Research Use Only” note in Product Data.
Item-specific notes:
Purity percentage, stabilizers, residual solvent limits, metal content, water/peroxide content, and UV cutoffs are not specified for this item; refer to CoA/Spec Sheet.
If your application requires low-background UV absorbance (e.g., LC-UV quantitation) or specific impurity thresholds, request the current CoA and analytical data package (HPLC/UPLC trace, NMR, MS) for your lot.
Reaction and Applications
This product is a finished small-molecule research tool, not a general-purpose synthetic reagent. Consequently, it is not typically used as a reactant in routine transformations.
Research applications (general, non-clinical):
As a reference inhibitor in biochemical kinase assays (e.g., enzymology, binding kinetics, thermal shift/DSF, nanoBRET target engagement).
As a positive control in cell-based signaling studies requiring modulation of specific tyrosine kinase pathways.
In ADME profiling (microsomal stability, permeability, plasma protein binding) as a comparator compound in medicinal chemistry campaigns.
Practical tips (general):
Prepare 10–50 mM DMSO stocks, aliquot, and store at −80°C to minimize freeze–thaw.
Validate activity in your assay matrix via a fresh dilution series, monitoring DMSO carryover and adsorption to plastics (consider low-bind consumables).
For biochemical assays, include detergent (e.g., 0.01% Tween-20) if nonspecific aggregation is suspected; confirm with counterscreens.
Reaction Conditions
Not typically applicable. Masitinib (AB1010) is a finished bioactive small molecule rather than a reagent used in chemical transformations.
Assay preparation conditions (general, for research use):
Stock solution: dissolve in DMSO to 10–50 mM; vortex and, if needed, sonicate briefly. Filter sterilize (0.2 µm) for cell culture assays if required.
Working concentrations: prepare serial dilutions in assay buffer or media; keep final DMSO ≤0.5–1% v/v to minimize solvent effects.
Pre-incubation: allow 10–30 min with enzyme or cells to reach binding equilibrium prior to initiating reactions (e.g., ATP addition in kinase assays).
These are generalized practices; optimize for your specific target, matrix, and readout.
Safety and Handling
GHS classification (item-specific): Not specified for this item; refer to SDS.
Signal word, pictograms, H-statements (item-specific): Not specified for this item; refer to SDS.
General laboratory safety guidance for small-molecule kinase inhibitors (not item-specific):
Handle in a chemical fume hood; avoid inhalation, ingestion, and skin/eye contact. Use appropriate PPE: lab coat, safety glasses, and nitrile gloves. Change gloves frequently when handling DMSO solutions.
Avoid generating dust or aerosols when weighing solids. Clean spills with inert absorbent, disposing in accordance with institutional and local regulations.
Storage incompatibilities: keep away from strong oxidizers and reactive acids/bases unless performing controlled salt formation. Avoid prolonged exposure to light and moisture.
First aid (overview; defer to SDS for authoritative instructions):
Skin/eye contact: rinse with water for ≥15 minutes; remove contaminated clothing; seek medical attention as needed.
Inhalation: move to fresh air; seek medical attention if symptoms persist.
Ingestion: rinse mouth; do not induce vomiting; seek medical attention.
Special risks:
Many kinase inhibitors are bioactive at low concentrations; minimize exposure and prevent environmental release.
DMSO solutions can enhance dermal absorption—use particular care to avoid skin contact.
Always consult the official SDS for the specific lot before use.
Solvent Selection
Masitinib is a hydrophobic/basic small molecule commonly prepared as concentrated DMSO stocks for screening.
PEG400 or Captisol blends: enable higher aqueous content for in vivo method development (research only), but can complicate LC-MS.
Always perform a micro-scale solubility check and filter (0.2 µm) before critical assays.
Storage and Reconstitution
Storage (item-specific): Store at −80°C.
Shipping (item-specific): Shipped on dry ice packs + cold packs.
Reconstitution and handling (general research guidance; not item-specific):
Allow container to equilibrate to room temperature in a desiccator before opening to avoid moisture condensation.
Prepare a concentrated DMSO stock solution (e.g., 10–50 mM). Vortex until fully dissolved; gentle warming (≤40°C) or brief sonication may assist.
Optional: Filter sterilize (0.2 µm PTFE) for cell-based work. Dispense into single-use aliquots in low-bind tubes to avoid adsorption and freeze–thaw.
Storage of solutions: keep aliquots at −80°C protected from light. Avoid repeated freeze–thaw; discard aliquots after a limited number of uses or if precipitation/degradation is observed.
Stability: Item-specific solution/solid-state stability data are not specified for this item; refer to CoA/Spec Sheet. Perform periodic QC (e.g., LC-MS) on working stocks used in critical studies.
For precise reconstitution instructions and stability limits for your lot, consult the CoA/SDS.
Structure and Identity
Masitinib (AB1010) is a research-grade, small-molecule kinase inhibitor commonly used as a reference compound in biochemical and cell-based studies.
Item-specific identifiers (from Product Data):
SKU: M409036
CAS: 790299-79-5
Grade: Moligand™
InChIKey: Not specified for this item; refer to CoA/Spec Sheet.
SMILES: Not specified for this item; refer to CoA/Spec Sheet.
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 (general/literature-level description, not item-specific):
Small-molecule ATP-competitive kinase inhibitor scaffold with multiple aromatic rings and heteroatoms.
Contains at least one basic tertiary amine functionality (commonly contributes to DMSO solubility and salt formation) and heteroaryl motifs typical of type II/III kinase inhibitors.
The 2D structure can be described qualitatively as a multi-ring, heteroatom-rich framework with an anilide/arylamide linkage and a basic side chain; no stereocenters are typically present in the free base.
Notes:
For definitive structural identifiers used for regulatory or analytical purposes at your site, please consult the product CoA/SDS or an authenticated reference standard.
Synthetic Utility
This product is supplied as a finished small molecule for biological research and analytical reference. It is not commonly used as a building block in general organic synthesis.
If chemical modification is pursued (research only), approaches may include:
Derivatization at the basic amine to form salts or quaternary ammonium derivatives for analytical probes.
Installation of reporter tags (e.g., biotin, fluorophores) via linkers when a suitable functional handle is present, to enable pull-down or imaging studies.
Such modifications require bespoke route design and may affect binding affinity and selectivity; they are outside the scope of standard reagent use.
For preparative synthetic chemistry needs, consider acquiring intermediate building blocks or starting materials rather than modifying the final inhibitor.
Target Specificity
Item-specific target, epitope, clone/isotype, or species reactivity data are not provided for this listing.
Target/assay specificity (item-specific): Not specified for this item; refer to CoA/Spec Sheet.
For literature-based information on biochemical selectivity panels and potency values, consult peer-reviewed sources and validate under your assay conditions.
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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