PF-04802367 - 10mM in DMSO , CAS No.1962178-27-3

CAS: 1962178-27-3 Cat. No.: P654675 Formula: C₁₆H₁₆ClN₅O₃ Molecular Weight: 361.78 EC Number: 110-369-0

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC 50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms ( GSK-3α and GSK-3β ) with IC 50 values of 10.0 and 9.0 nM in mobility shift assays, respectively

In Vitro

PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity in vitro with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively. PF-367 has reasonable in vitro stability in human hepatic microsomes (t 1/2 =78.7 min), has excellent passive permeability. In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC 50 of 466 nM. PF-367 has good cell viability (IC 50 of 117 μM in THLE cytotoxicity assays) and an IC 50 >100 μM in a hERG screening assay. PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC 50 of 6.2 μM, gene transcription in U20S cells with EC 50 of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC 50 of 9.0 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent . PF-04802367 (PF-367), a potent type-I dual GSK-3α/β inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats Dosage: 1, 3.2, 10, 32 or 50 mg/kg Administration: A single subcutaneous Result: Inhibition of phosphorylation of tau in brain is dose-dependent.

IC50& Target:GSK-3α 10 nM (IC 50 ) GSK-3β 9 nM (IC 50 )

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC 50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay.xa0PF-04802367 shows desirable central nervous system (CNS)xa0properties and potency. PF-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

Molecular Weight

361.78

Application Protocols

No tested applications or validated protocols are provided in the Product Data for PF-04802367. The following is general, non-item-specific guidance for handling small-molecule test articles in research assays:

General assay workflow (non-validated template):

• Preparation: Equilibrate vial to room temperature in a desiccator before opening. Prepare a 10–50 mM stock in anhydrous DMSO. Vortex/sonicate to fully dissolve.
• Aliquoting: Dispense single-use aliquots (10–50 μL) into low-bind microtubes or plates. Store at −80°C. Avoid repeated freeze–thaw.
• Dilution: Thaw an aliquot on ice or at room temperature, then dilute into assay buffer to the desired final concentration, keeping DMSO constant across controls.
• Controls: Include vehicle control (matching DMSO%), positive/negative controls where relevant, and a serial dilution series (e.g., 1:3 or 1:2) for potency curves.
• Quality checks: Inspect for precipitation/turbidity. Optionally confirm concentration by UV or LC where extinction coefficients or reference curves are available.
• Data integrity: Randomize plate layout to minimize edge effects; include replicates (≥3 technical) and at least two biological repeats where feasible.

These steps are intended as general best practices; they do not constitute item-specific validated protocols.

Biological Roles

Target, mode-of-action, and biological role data are not provided in the Product Data for PF-04802367. Consequently, no item-specific biological functions can be stated here.

General context for small-molecule research compounds (non-item-specific, literature-based):

• Such compounds may act as enzyme inhibitors, receptor ligands, ion channel modulators, or pathway probes in discovery research; however, the specific biological interactions of PF-04802367 are not specified.
• In early research workflows, compounds are characterized by potency (e.g., IC50/EC50), selectivity panels, and ADME properties. These values—if available—should be taken from peer-reviewed literature or the item’s CoA; none are provided here.
• Off-target liability and assay interference (e.g., redox cycling, aggregation) must be assessed empirically. Counter-screens and detergent controls can help identify nonspecific effects.

Research-use-only notice:

• This product is for research use only, not for human or veterinary use, diagnostic procedures, or clinical applications. No therapeutic or clinical claims are made or implied.

For any biological role or target specificity, consult independent literature sources using the CAS (1962178-27-3) or request additional documentation. Absent such sources, treat PF-04802367 as a compound of unknown biological role.

Buffer Applications

PF-04802367 is not a buffering agent and is not intended to establish or maintain pH in solutions.

Practical notes for assay buffers (general guidance, not item-specific specifications):

• Vehicle control: Match the DMSO (or other solvent) concentration across all wells/samples to the highest test concentration (commonly ≤0.1–0.5% v/v).
• Order of addition: Add compound stock last into pre-equilibrated buffer with vigorous mixing to minimize local supersaturation and precipitation.
• Common assay buffers: HEPES (pH 7.2–7.5), PBS, or Tris (pH 7.4–8.0) depending on target biology; ensure compatibility if the compound is pH-sensitive (unknown for this item).
• Surfactants and carriers: Low levels of nonionic surfactants (e.g., 0.01–0.05% Tween-20 or Pluronic F-127) can mitigate colloidal aggregation for certain chemotypes; evaluate case-by-case.

Buffer recipes or pKa-based buffering ranges are not applicable to this compound due to the absence of acid/base buffering functionality information. Refer instead to Storage & Reconstitution and Solvent Selection for practical handling in assay environments.

Green Alternatives

As a discrete screening compound, PF-04802367 is used at micro- to milligram scales; the major environmental considerations arise from solvent handling rather than bulk reagent substitution.

Greener handling strategies (general guidance):

• Prefer lower-toxicity, lower-VOC solvents for preparative steps around the compound (e.g., ethanol or 2-propanol for vial rinsing) when compatible with the chemistry.
• For stock solutions, DMSO is common but has a high boiling point; minimize waste and consolidate rinses. If solubility allows, ethanol or aqueous co-solvent systems may reduce DMSO use.
• Scale down experiments and adopt miniaturized assay formats (384/1536-well) to reduce solvent consumption.
• Implement closed-container thawing and precise aliquoting to limit material loss and subsequent solvent-intensive cleanup.

Illustrative comparison (general; not item-specific):

• DMSO vs ethanol for stock preparation
  • Solubility: DMSO typically higher; ethanol moderate.
  • Assay compatibility: Both can be acceptable at ≤0.1–0.5% v/v; verify.
  • Environmental profile: Ethanol generally considered greener; choice depends on solubility and assay constraints.

Waste minimization:

• Collect organic solvent waste by compatibility class; segregate halogenated from non-halogenated streams.
• Use microvolumes and automated liquid handling to reduce overage. Validate shortest feasible incubation times to cut energy use for temperature control.

No item-specific green certifications or solvent requirements are provided for this product.

Pharmaceutical Uses

No pharmacopeial status, excipient role, or formulation use is provided for PF-04802367. This product is supplied strictly for research use only.

Clarifications (non-clinical, non-therapeutic):

• Not an approved API, not listed as a compendial excipient, and not intended for any clinical or diagnostic application.
• If used as a research reference standard or tool compound in preclinical experiments, ensure appropriate documentation of purity, identity, and stability (via CoA and in-house QC) before use.

Formulation considerations for research assays (general guidance):

• Typical approach involves preparing concentrated DMSO stocks and diluting into in vitro assay media; final solvent content should be validated for biological tolerance.
• For in vivo preclinical research (if performed under appropriate approvals), formulation strategies might include co-solvents, cyclodextrins, or lipid-based vehicles; however, no item-specific formulation data are provided or implied here.

Regulatory and safety note:

• Any translation of research findings to regulated studies would require comprehensive CMC characterization, GLP/GMP sourcing, and toxicology—none of which are covered by this research-use-only material.

Physical Properties

Item-specific physicochemical properties are not provided in the current Product Data.

• Appearance: Not specified for this item; refer to CoA/Spec Sheet.
• Melting point (MP): Not specified for this item; refer to CoA/Spec Sheet.
• Boiling point (BP): Not applicable/unknown for solids; Not specified for this item; refer to CoA/Spec Sheet.
• Density: Not specified for this item; refer to CoA/Spec Sheet.
• LogP/logD, pKa, refractive index: Not specified for this item; refer to CoA/Spec Sheet.
• Solubility: Not specified for this item; refer to CoA/Spec Sheet.

General laboratory guidance (literature/practice, not item-specific specifications):

• Small-molecule screening compounds are commonly reconstituted as concentrated stock solutions in anhydrous DMSO (e.g., 10–50 mM), with subsequent dilution into assay buffers keeping final DMSO ≤0.1–0.5% v/v where assay-compatible.
• Empirical solubility testing can be performed via serial dilution and visual turbidity/precipitation checks, supplemented by nephelometry or UV/UPLC quantitation.
• For ionizable compounds, co-solvent systems (DMSO/water, DMSO/ethanol) or pH adjustment of aqueous media may enhance solubility; filter sterilization through 0.22 μm PTFE/nylon can clarify micro-particulates if chemistry is compatible.
• Light and moisture sensitivity should be assumed until proven otherwise; protect solutions from light and avoid repeated freeze–thaw cycles.

All numerical specifications that are not explicitly provided here are not specified for this item; refer to CoA/Spec Sheet.

Quality & Grades

Grade/purity are not specified for this listing; consult the CoA/Spec Sheet for lot-specific details.

• Grade/Purity: Not specified for this item; refer to CoA/Spec Sheet.
• Stabilizers/antioxidants: Not specified for this item; refer to CoA/Spec Sheet.

Context and expectations (general guidance for small-molecule research compounds):

• Discovery compounds in screening libraries are typically supplied at high chemical purity (often ≥95% by HPLC/UPLC), with identity confirmed by MS and/or NMR. However, this is not specified for this particular SKU and should be verified on the CoA.
• For bioassay use, low levels of residual solvents, reagents, and salts are desirable to minimize assay interference. Confirm residual solvent profile by GC or HS-GC when critical.
• If optical purity is relevant (chiral centers), request enantiomeric or diastereomeric purity data (e.g., chiral HPLC) from the CoA. Absent such data, assume racemic or unspecified configuration.
• UV-cutoff and LC-MS transparency: Not specified for this item; refer to CoA/Spec Sheet. For chromatographic detection method development, run a short scout gradient to assess UV response and ionization efficiency.

Documentation and traceability:

• Keep a copy of the lot-specific CoA and SDS in your ELN/LIMS. Record internal QA checks (HPLC% area, LC-MS, NMR) upon receipt to ensure fitness-for-purpose in your assays.

Reaction & Applications

This product is positioned as a small-molecule research compound rather than a general-purpose synthetic reagent. No item-specific synthetic or catalytic application data are provided.

Applicable use domain (general, non-item-specific):

• As a reference or test article in biochemical, biophysical, or cellular assays within screening cascades and SAR workflows.
• Tool compound evaluation in phenotypic screens or target-based assays, contingent on verified identity/purity and literature knowledge (if available from independent sources). No target specifics are provided for this item.

Not typically applicable:

• It is not primarily intended for named reactions, stoichiometric reagents, or catalysts in preparative organic synthesis. For such needs, select purpose-built reagents with defined specifications.

Practical guidance for assay deployment (general):

• Prepare anhydrous DMSO stocks; confirm solubility and absence of precipitation upon aqueous dilution.
• Use vehicle controls matched for DMSO percentage across all wells/samples.
• Where possible, include orthogonal assay formats (e.g., biochemical vs cell-based) to de-risk assay artifacts.
• Confirm stability in assay media (time-course LC/UPLC) to rule out rapid hydrolysis/oxidation.

All application claims specific to PF-04802367 are not specified for this item; refer to CoA/Spec Sheet and independent literature if available.

Reaction Conditions

Reaction condition guidance is not applicable because PF-04802367 is not presented as a reagent or catalyst and its structure is not provided.

Where relevant to assay preparation (general, not item-specific specifications):

• Stock solution preparation: Dissolve in anhydrous DMSO at a concentration suitable for your assay (commonly 10–50 mM), vortex and, if necessary, sonicate briefly to aid dissolution.
• Aqueous dilution: Add stock slowly into buffered media with mixing; verify absence of precipitation by visual inspection or nephelometry.
• Stability checks: Perform short-term stability assessments at intended assay temperature (e.g., 25–37°C) over the assay timeframe using UPLC/UV or LC-MS.

No temperatures, catalysts, or yields can be recommended for chemical reactions involving PF-04802367 due to the absence of structural and reactivity information. For chemical transformations, obtain full structural data and consult reaction-specific literature.

Safety & Handling

Hazard classification details are not provided in the Product Data for this item. Treat as a laboratory chemical of unknown toxicity and follow standard precautions.

• GHS classification, pictograms, H-statements: Not specified for this item; refer to SDS.
• Signal word: Not specified for this item; refer to SDS.

General safety guidance (consult SDS for authoritative instructions):

• PPE: Use lab coat, safety glasses, and appropriate chemical-resistant gloves (e.g., nitrile). Handle powders and DMSO solutions in a fume hood to minimize inhalation/dermal exposure and DMSO-facilitated skin uptake.
• Avoid generating dust or aerosols. Use closed microtubes or crimp-sealed vials for storage and thawing. Allow vials to equilibrate to room temperature in a desiccator before opening to prevent condensation.
• Incompatibilities: Absent item-specific data, avoid strong oxidizers and strong acids/bases until compatibility is confirmed. Do not heat or evaporate to dryness without understanding thermal properties.
• First aid overview: If inhaled—fresh air and medical attention if symptoms occur. Skin/eye contact—immediately wash with water for at least 15 minutes; remove contaminated clothing. If swallowed—rinse mouth; seek medical advice. Provide SDS to healthcare personnel.
• Waste: Collect in halogenated or non-halogenated organic waste streams per local regulations; decontaminate surfaces with suitable organic solvent or detergent solution.

Storage note: Store at −80°C as provided in the Product Data. Keep container tightly closed, dry, and protected from light. Always defer to the SDS for definitive safety information.

Solvent Selection

Item-specific solubility data are not provided. The following are general, literature-based best practices for small-molecule screening compounds and should be verified empirically for PF-04802367.

Primary reconstitution choices (general):

• DMSO (anhydrous): Common first-line solvent for preparing concentrated stocks (e.g., 10–50 mM). Offers broad solubility for heteroaromatic and polycyclic scaffolds.
• DMF or NMP (anhydrous): Alternative high-boiling polar aprotic solvents if DMSO solubility is inadequate. Consider assay compatibility and extraction from aqueous media.
• Ethanol/MeOH: Useful for moderately lipophilic or neutral compounds; typically limited to lower stock concentrations vs DMSO.

Aqueous dilution guidance:

• Dilute DMSO stocks into pre-warmed assay buffer with vigorous mixing to minimize precipitation; maintain final DMSO ≤0.1–0.5% v/v where biologically compatible.
• Solubility enhancers (if compatible with assay): 0.01–0.05% nonionic surfactant (e.g., Tween-20 or Pluronic F-127), ≤5% co-solvent (ethanol or PEG-400), or adjusted pH if ionizable.

Small comparison (general considerations):

• DMSO: Highest solvating power; potential to enhance dermal absorption—use care.
• Ethanol: Biologically tolerated at low %; lower solubility ceiling.
• DMF/NMP: Strong solvents but with stricter handling/SDS considerations.

Practical tips:

• Filter stocks only if chemistry is compatible (PTFE syringe filters); some compounds adsorb to filter media.
• Aliquot stocks to avoid repeated freeze–thaw; store at −80°C per Product Data.

Storage & Reconstitution

Item-specific storage and shipping information are provided; all other details should be verified against the CoA/SDS.

• Storage conditions (item-specific): Store at −80°C.
• Shipped in (item-specific): Dry ice packs + cold packs.
• Appearance: Not specified for this item; refer to CoA/Spec Sheet.
• Stability/expiry: Not specified for this item; refer to CoA/Spec Sheet.

Reconstitution guidance (general best practices for small molecules):

• Solvent: Use anhydrous DMSO as the first choice for stock solutions unless solubility data indicate otherwise. Alternative solvents (DMF, ethanol) may be considered based on compatibility and solubility.
• Concentration: Common research stock concentrations are 10–50 mM; determine empirically to avoid precipitation upon aqueous dilution.
• Technique: Allow vial to reach room temperature in a desiccator before opening to prevent moisture condensation. Vortex and, if needed, brief sonication to aid dissolution. Protect from light if the compound is light-sensitive (unknown for this item).
• Aliquoting: Prepare single-use aliquots in tightly sealed, low-bind tubes or capped vials. Minimize headspace and moisture ingress.
• Freeze–thaw: Avoid repeated freeze–thaw cycles; discard thawed, unused portions to maintain integrity.

All non-specified parameters (water content, peroxide levels, metal content, UV cutoff, etc.) are not specified for this item; refer to CoA/Spec Sheet.

Structure & Identity

PF-04802367 is listed as a small-molecule research compound in our small-molecule and compound library category. Item-specific structural identifiers are not provided in the Product Data for this SKU.

• CAS: 1962178-27-3 (item-specific)
• Chemical name: Not specified for this item; refer to CoA/Spec Sheet.
• Synonyms: 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.
• SMILES: Not specified for this item; refer to CoA/Spec Sheet.
• InChIKey: Not specified for this item; refer to CoA/Spec Sheet.

Structural features (general guidance):

• As a coded discovery compound (PF- prefix), PF-04802367 likely represents a discrete organic scaffold optimized for a biological target; however, the exact functional groups, ring systems, and stereochemistry are not provided here and should be confirmed from the CoA/SDS or primary literature.
• Without a provided structure, no 2D/3D depiction, stereochemical description, or functional-group inventory can be asserted for this specific lot.

Identity confirmation (general best practices):

• For research authentication, confirm identity by orthogonal methods such as high-resolution MS, 1H/13C NMR, and HPLC/UPLC purity profiling.
• If an internal reference standard is available, compare retention time and MS fragmentation patterns under matched chromatographic conditions.
• For biological assays, verify potency benchmarks (if known from literature) only after analytical confirmation of identity and purity. All item-specific identifiers beyond CAS are currently not specified for this item; refer to CoA/Spec Sheet.

Synthetic Utility

PF-04802367 is offered as a discrete research compound, not as a general synthetic building block or reagent. No functional-group detail, reactivity, or protecting-group compatibility is provided in the Product Data.

Accordingly, traditional "synthetic utility" guidance (e.g., use as a coupling partner, nucleophile/electrophile, catalyst ligand) is not applicable without structural information.

General considerations for chemists (non-item-specific):

• If derivatization or SAR exploration is anticipated, obtain structural information (SMILES/InChI) and assess positions amenable to modification, liability motifs, and stability under standard transformations (oxidation/reduction, cross-coupling, amide formation, etc.).
• Assess stability under common workups (acid/base, aqueous quench) and purifications (silica gel, basic alumina, reverse-phase chromatography) only after structure is confirmed.

For this SKU, no statements can be made about reactive handles, heteroatom content, metal-binding motifs, or stereochemical lability. Please refer to the CoA/Spec Sheet or original literature for structural and reactivity guidance.

Target Specificity

No target, pathway, or binding specificity information is provided in the Product Data for PF-04802367.

• Target/Pathway: Not specified for this item; refer to CoA/Spec Sheet.
• Species reactivity or cell-line context: Not specified for this item; refer to CoA/Spec Sheet.
• Assay-validated endpoints or biomarkers: Not specified for this item; refer to CoA/Spec Sheet.

Guidance (general, not item-specific claims):

• If target specificity is available from independent literature (using the CAS 1962178-27-3), validate activity under your experimental conditions with appropriate positive/negative controls and orthogonal readouts.
• Consider panel screening to evaluate selectivity and off-target profiles before advanced studies.

In the absence of item-specific data, treat PF-04802367 as a compound of unknown specificity.

Frequently Asked Questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1962178-27-3, the molecular formula is C16H16ClN5O3, and the molecular weight is 361.78 g/mol.

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.