QUALITÄT & REINHEITMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.≥99%
FIIN-3 is an irreversible inhibitor of FGFR with an IC 50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1 , FGFR2 , FGFR3 and FGFR4 , respectively.
In Vitro
FIIN-3 potently inhibits both WT FGFRs (EC 50 in the 1- to 41-nM range) and the gatekeeper mutant of FGFR2 (EC 50 of 64 nM). FIIN-3 also strongly inhibits EGFR, with an EC 50 of 43 nM. FIIN-3 shows good potency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutant E565K; FIIN-3 also displays antiproliferative activity (with an EC 50 of 135 nM) against Ba/F3 cells transformed by the EGFR vIII fusion protein, which has a WT EGFR kinase domain. FIIN-3 shows even better activity against EGFR mutant L858R (EC 50 of 17 nM) and moderate activity, displaying an EC 50 of 231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completely inhibits the FGFR2 autophosphorylation on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564M Ba/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partial inhibition at 100 nM and complete inhibition observed at 300 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl 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
Only product-data-derived protocols are permitted in this section.
Tested applications, recommended dilutions, and positive controls: Not specified for this item; refer to CoA/Spec Sheet.
General reminder:
Establish assay-specific standard operating procedures and validate concentration ranges, incubation times, and vehicle controls under your laboratory conditions.
Biological Roles
All statements below are for research context only. No medical or clinical claims are made.
Literature characterization of FIIN-class probes:
Target class: Fibroblast growth factor receptors (FGFR1–4), a family of receptor tyrosine kinases central to FGF signaling in development, metabolism, and tissue homeostasis.
Modality: Irreversible (covalent) kinase inhibition via a Michael acceptor that forms a bond with a conserved cysteine residue in the ATP-binding site (literature). This can provide sustained target engagement in cellular systems.
Research uses: Dissecting FGFR-driven phosphorylation cascades (e.g., FRS2, ERK, AKT), modeling resistance and bypass signaling, and validating FGFR dependence in engineered cell lines or biochemical systems.
Probe-type considerations: Covalent inhibitors facilitate washout-resistant phenotypes in time-course studies and can aid chemoproteomic target confirmation when paired with competition or mutant controls.
Caveats (general):
Off-target reactivity can occur with other cysteine-containing kinases; comprehensive profiling under your assay conditions is recommended.
Potency and selectivity are assay- and context-dependent; buffer composition, ATP concentration, and protein constructs can shift apparent IC50 values.
Item-specific bioactivity data (potency, Kd/IC50, kinome selectivity): Not specified for this item; users should consult primary literature and/or generate internal benchmarking with appropriate controls.
Buffer Applications
This compound is a small-molecule probe and does not serve as a buffering agent. No acid/base equilibria suitable for pH control are provided in this listing.
Practical notes for using FIIN-3 in buffered assays (general):
Prepare concentrated DMSO stocks and dilute into pre-warmed assay buffer (e.g., PBS, HEPES, or cell culture media) to achieve the desired final concentration while keeping DMSO ≤0.1–1% v/v, as assay tolerance allows.
To minimize precipitation, add the DMSO stock slowly with vigorous mixing; include a small amount of carrier protein (e.g., 0.1% BSA) or non-ionic surfactant (e.g., 0.01–0.05% Tween-20) if compatible with the assay.
Avoid prolonged exposure at elevated temperature or alkaline pH, which can promote undesired reactions of electrophilic motifs (general caution for covalent probes).
Item-specific buffer compatibility or pKa values: Not specified for this item; refer to CoA/Spec Sheet and verify empirically under your assay conditions.
Green Alternatives
This listing is a bioactive probe, not a process solvent or bulk reagent; “green alternatives” are therefore not directly applicable to the product itself. Nevertheless, greener handling strategies can be applied to its use in research workflows.
Greener handling strategies (general):
Prefer DMSO for stock solutions over halogenated solvents (e.g., dichloromethane, chloroform) or high-toxicity polar aprotics.
Minimize solvent volumes via concentrated DMSO stocks (e.g., 10–50 mM) and microvolume dispensing.
Use aqueous buffer systems with low percentages of co-solvent, and avoid unnecessary pH adjustments that can induce degradation.
Consolidate solvent waste from screening campaigns and segregate halogenated from non-halogenated streams to facilitate compliant disposal.
If performing custom synthesis or analog preparation (general):
Consider greener reaction media (e.g., 2-MeTHF, CPME, EtOAc) and catalytic methods when feasible.
Apply solvent selection guides (e.g., CHEM21, ACS GCI) for chromatography and workup to reduce environmental impact.
Trade-offs:
Highly hydrophobic probes may require some organic co-solvent to avoid precipitation; balance environmental goals with data quality and compound integrity.
Pharmaceutical Uses
This product is supplied strictly for research use only. It is not an API, excipient, or GMP material, and is not intended for human or veterinary use.
Context for formulation scientists (general, non-clinical):
As a research probe, FIIN-3 may be formulated into DMSO or mixed-solvent vehicles for in vitro assays. For in vivo exploratory studies within regulated institutions, formulation development (e.g., cosolvent/surfactant systems) should be performed using institutionally approved protocols and materials; this catalog entry provides no such specifications.
Item-specific pharmacopeial status, residual solvent profile, or excipient compatibility: Not specified for this item; refer to CoA/Spec Sheet if available, and conduct independent qualification as required by your institution.
Compliance reminder:
No clinical, diagnostic, or therapeutic applications are supported or implied. Handle under research laboratory quality systems only.
Physical Properties
Item-specific physico-chemical specifications are not listed for this catalog entry. Do not infer performance-critical values from generic sources; use the lot-specific CoA where available.
Physical state/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 for typical solid probe compounds; Not specified for this item.
Density: Not specified for this item; refer to CoA/Spec Sheet.
Solubility:
Aqueous: Not specified for this item; many kinase probes exhibit low intrinsic water solubility (literature generality).
Organic: Frequently formulated in anhydrous DMSO for stock solutions (literature/general practice).
LogP/logD: Not specified for this item; refer to CoA/Spec Sheet or cheminformatics calculation.
pKa: Not specified for this item; refer to CoA/Spec Sheet or literature.
UV-Vis λmax: Not specified for this item; refer to CoA/Spec Sheet.
Refractive index: Not applicable for solids; Not specified for this item.
Practical guidance (general):
Prepare concentrated stocks in dry DMSO (e.g., 10–50 mM) and dilute into assay buffers immediately before use to minimize precipitation; include ≤0.1–1% final DMSO in biological assays, as tolerance permits (literature/common practice).
If precipitation is observed upon dilution, increase dilution temperature slightly, add a small co-solvent fraction (e.g., PEG-400 or ethanol), or reduce working concentration.
Quality and Grades
Grade: Moligand™ (item-specific). Moligand™ denotes inclusion in a curated small-molecule/ligand collection intended for target-engagement and pathway interrogation in research settings. Emphasis is placed on chemical identity, integrity, and fitness for chemical biology workflows.
What Moligand™ typically implies (general):
Verified identity by orthogonal analytical methods (e.g., NMR/HRMS/LC). Exact acceptance criteria are lot-specific; consult the CoA.
Purity optimized for biological screening and mechanistic studies. If precise purity (HPLC area %, residual solvent/metals) is critical for your protocol, request the CoA/specification sheet. Do not assume unstated limits.
Packaging to preserve stability (light protection, low-temperature shipment).
Item-specific facts:
Purity value: Not specified for this item; refer to CoA/Spec Sheet.
Stabilizers/additives: Not specified for this item; refer to CoA/Spec Sheet.
Identity release tests and analytical method details: Not specified for this item; refer to CoA/Spec Sheet.
Recommendations for QC on receipt (best practice):
Inspect for integrity (no discoloration, clumping, or container breach).
Record mass and appearance; if needed, perform a quick LC-UV or LC-MS check in your in-house system to confirm retention time and purity under your assay conditions.
Reaction and Applications
This product is a bioactive small-molecule probe, not a synthetic reagent or solvent. Accordingly, classical synthetic “reaction applications” (e.g., use as a base, ligand, or coupling partner) do not apply.
Research applications (general, literature-based for FIIN-class probes):
Target engagement studies of FGFR family kinases using biochemical enzymatic assays, NanoBRET/kinase tracer displacement, or CETSA/TPP workflows.
Pathway interrogation in cells: modulation of FGFR signaling to study downstream ERK/AKT pathway responses, feedback, and resistance mechanisms.
Chemoproteomics: leveraging the electrophilic warhead to assess covalent target occupancy on cysteine-containing kinases and potential off-target profiling.
Structure–activity relationship (SAR) benchmarking alongside related scaffolds to refine potency/selectivity in medicinal chemistry programs.
Assay design tips (general):
Establish DMSO-only vehicle controls matching the highest solvent concentration used.
Perform short pre-incubations (e.g., 15–60 min) for covalent occupancy studies before stimulation or lysis, as appropriate for the assay format.
Include washout controls to differentiate reversible binding from covalent target engagement.
Note: No item-specific activity data, potency values (IC50/Ki), or selectivity panels are provided in this listing; consult primary literature and/or generate in-house data under your assay conditions.
Reaction Conditions
Not applicable. FIIN-3 is not intended for use as a reagent in chemical transformations, so typical “reaction conditions” (catalysts, temperatures, yields) are not relevant to its end use as a probe.
For biological experiments (general guidance; literature/common practice):
Stock solutions: 10–50 mM in anhydrous DMSO; store as aliquots at −20°C, protected from light.
Working concentrations: commonly tested in the low nanomolar to low micromolar range depending on assay type and target expression; determine empirically.
Incubation: allow sufficient pre-incubation for covalent engagement (e.g., 15–60 minutes) before endpoint measurements.
Item-specific kinetic parameters (kinact/Ki), potency, and stability in specific media: Not specified for this item; users should establish these under their conditions and consult primary literature for initial benchmarking.
Safety and Handling
Authoritative safety guidance is provided in the product SDS. This section gives general laboratory best practices for small-molecule kinase probe compounds.
GHS classification, signal word, pictograms, H-statements: Not specified for this item; consult the SDS for the shipped lot.
Likely hazards (general): Organic research chemicals may cause skin/eye irritation and may be harmful if swallowed or inhaled. FIIN-3 contains an electrophilic warhead (literature), which can alkylate nucleophiles; avoid contact.
Handling and PPE:
Use in a chemical fume hood.
Wear appropriate PPE: lab coat, safety glasses, and chemically resistant gloves (e.g., nitrile). Change gloves regularly when handling DMSO solutions (enhanced dermal transport risk).
Storage and stability:
Store at −20°C, protected from light (item-specific).
Keep container tightly closed; minimize freeze–thaw by aliquoting DMSO stocks.
Incompatibilities and precautions (general):
Avoid strong bases/nucleophiles during storage of solutions, which may consume the electrophile.
Avoid prolonged exposure to moisture and elevated temperatures.
First aid (summary; defer to SDS):
Skin/eye contact: Rinse with water for 15 minutes; remove contaminated clothing; seek medical attention if irritation persists.
Inhalation: Move to fresh air; seek medical attention if symptoms occur.
Ingestion: Rinse mouth; do not induce vomiting; seek medical attention.
Waste disposal:
Treat as hazardous organic waste; follow institutional and local regulations.
Solvent Selection
FIIN-3 is used as a small-molecule probe, not as a reaction solvent. Solvent considerations therefore focus on dissolving, storing, and dosing the compound into assays.
General solubility guidance (literature/common practice for kinase probes):
Primary stock solvent: Anhydrous DMSO (high solvating power, miscible with aqueous buffers upon dilution).
Secondary co-solvents for staged dilution: ethanol, acetonitrile, or PEG-400 (small fractions) to mitigate precipitation in aqueous media.
Aqueous buffers: Use assay buffer with protein/serum or surfactant (e.g., 0.01–0.05% Tween-20) to aid dispersion when needed.
Polarity/miscibility profile (general):
DMSO stocks are miscible with water, PBS, and most biological buffers; maintain final DMSO typically ≤0.1–1% v/v to balance solubility and biological tolerance.
Practical tips:
Warm buffer to ambient temperature before adding the DMSO stock; add stock slowly with vortexing.
Prepare serial dilutions in DMSO before aqueous dilution to improve accuracy at low nanomolar–micromolar working concentrations.
Filter sterilize only if necessary; many small molecules may adsorb to filters—validate recovery.
Comparison (general):
DMSO vs DMF: DMSO offers better biocompatibility for cell assays; DMF can be used for analytical sample prep but is less preferred for live-cell dosing.
DMSO vs ethanol: Ethanol is acceptable at low percentages; DMSO typically provides higher stock concentration and stability.
Storage and Reconstitution
Item-specific storage and shipping:
Storage Conditions: Store at −20°C, protected from light (item-specific).
Shipped In: Ice chest + Ice pads (item-specific) to maintain low temperature during transit.
Reconstitution (general best practice for small-molecule probes):
Allow vial to equilibrate to room temperature in a desiccated environment before opening to prevent moisture condensation.
Prepare a concentrated stock in anhydrous DMSO (e.g., 10–50 mM). Mix thoroughly to ensure complete dissolution. If necessary, sonicate briefly or warm gently (≤37°C).
Aliquot the stock into low-adsorption microtubes to minimize freeze–thaw cycles. Backfill with inert gas if extended storage is anticipated.
Store aliquots at −20°C, protected from light. Avoid repeated freeze–thaw; thaw only what is needed for immediate use.
Working solution preparation (general):
Dilute the DMSO stock into assay buffer or media with vigorous mixing to the desired final concentration, keeping DMSO typically ≤0.1–1% v/v based on assay tolerance.
Inspect for precipitation; if observed, reduce concentration, add a small co-solvent fraction (e.g., ethanol or PEG-400), or adjust the dilution sequence.
Stability notes:
Item-specific stability in solution and sensitivity to pH/light are Not specified for this item; consult the CoA/SDS and verify empirically under your conditions.
Structure and Identity
Overview: FIIN-3 is a research-use small molecule from the Moligand™ collection, commonly referenced in the literature as a covalent FGFR pathway probe. Item-specific identifiers are limited in this listing; consult the CoA/SDS for definitive identifiers.
SKU: F650747
Product Name: FIIN-3
CAS: 1637735-84-2 (item-specific)
PubChem CID: 73707531 (item-specific)
InChIKey: 334587 (as provided; truncated/not standard — verify on CoA)
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):
FIIN-3 is widely described as an irreversible, cysteine-targeting kinase inhibitor scaffold with an electrophilic acrylamide (Michael acceptor) linked to a heteroaromatic ATP-competitive recognition motif. It is designed to target FGFR family kinases in their ATP-binding site.
Typical 2D description (literature): a multi-ring heteroaromatic core bearing an acrylamide or analogous electrophile, with halogen and/or polar substituents modulating potency and selectivity. Exact atom-by-atom connectivity should be taken from an authoritative database entry or the CoA.
Notes:
Where discrepancies exist between literature databases and this catalog entry, defer to the product CoA/SDS accompanying the shipped lot.
Synthetic Utility
FIIN-3 is supplied as a finished small-molecule probe, not as a reagent or intermediate. Consequently, it is not typically employed as a building block in routine organic synthesis.
General medicinal chemistry context (literature):
FIIN-class covalent FGFR inhibitors exemplify the strategic incorporation of an acrylamide electrophile onto a kinase-recognition scaffold. From a design perspective, they illustrate covalent warhead placement relative to the hinge-binding core and the targeted cysteine in the ATP pocket.
For synthetic method development or analoging, practitioners may explore late-stage functionalization on heteroaromatic cores, amide coupling to install the electrophile, and careful protection/deprotection strategies to maintain warhead integrity.
Item-specific synthetic or reactivity data (e.g., as a nucleophile/electrophile in bench reactions): Not applicable/not specified for this item.
If users intend to derivatize the scaffold (general advice):
Conduct reactions under anhydrous, low-base conditions to preserve the acrylamide.
Use orthogonal protecting groups to tolerate heteroaromatic substitutions, and verify warhead integrity by LC-MS/MS.
Target Specificity
Only product-data-derived specificity claims are permitted in this section.
Item-specific target, epitope, or selectivity panel: Not specified for this item; refer to CoA/Spec Sheet.
Note: While FIIN-class probes are discussed in the literature in the context of FGFR family kinases, no target claims are made here beyond what is provided in the product data.
Häufig gestellte Fragen
What is the purity of this product?
This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.
What is Moligand??
Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.
How should this product be stored?
Store at ?20 °C, protected from light. The material is light-sensitive — keep it in its original opaque or amber container.
How is this product shipped?
This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 1637735-84-2, the molecular formula is C34H36Cl2N8O4, and the molecular weight is 691.61 g/mol. InChIKey SFLKJNSBBVSPFE-UHFFFAOYSA-N.
What documentation is provided?
Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.
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