≥98% per flussi di lavoro cromatografici e analitici sensibili che richiedono un'interferenza minima della linea di base.
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Stoccaggio e spedizione
Store at -20°C Spedizione Ice chest + Ice pads. Consultare il COA specifico del lotto per le specifiche esatte.
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Documenti di qualità
SDS, COA, scheda tecnica e scheda delle specifiche disponibili per il download. COA specifico del lotto accessibile tramite ricerca per numero di lotto.
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Prova documentale
Citato in 0 pubblicazioni peer-reviewed su cromatografia, sintesi organica e reazioni di accoppiamento incrociato.
Panoramica
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 ( MDM2 ) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2 . MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC 50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent
In Vitro
MD-224 (1-30 nM; 2 hours) effectively induces depletion of MDM2 protein and concurrently accumulation of p53 protein in a dose-dependent manner in RS4;11 cells. MD-224 (30 nM; 6 hours) is more potent than MI-1061 in induction of transcriptional upregulation of these p53 target genes but have no effect on TP53 itself in RS4;11 cells. MD-224 (0.001-1 μM; 24 hours) induces robust apoptosis at ≤10 nM in a dose-dependent manner upon a 24 hours treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: RS4;11 cells Concentration: 1 nM; 3 nM; 10 nM; 30 nM Incubation Time: 2 hours Result: Decreased MDM2 protein and accumulated of p53 protein. RT-PCRCell Line: RS4;11 cells Concentration: 30 nM Incubation Time: 6 hours Result: Upregulated p53 target gene expression. Apoptosis AnalysisCell Line: RS4;11 cells Concentration: 0.001 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM Incubation Time: 24 hours Result: Induces robust apoptosis in RS4;11 cells.
Form:Solid
IC50& Target:MDM2 1 nM (IC 50 )
Specifiche
Specifiche e purezza
≥98%
Meccanismi biochimici e fisiologici
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 ( MDM2 ) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2 . MD-224 induces rapid degradation of M
Condizioni di conservazione di stoccaggio
Store at -20°C
Spedito in
Ice chest + Ice pads
Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.
Certificati (CoA, COO, BSE/TSE e tabella di analisi)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Proprietà chimiche e fisiche
Solubilità
DMSO : 100 mg/mL (112.38 mM; Need ultrasonic)
Peso molecolare
889.800 g/mol
XLogP3
5.900
Hydrogen Bond Donor Count
5
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
9
Exact Mass
888.261 Da
Monoisotopic Mass
888.261 Da
Topological Polar Surface Area
166.000 Ų
Heavy Atom Count
63
Formal Charge
0
Complexity
1880.000
Isotope Atom Count
0
Defined Atom Stereocenter Count
3
Undefined Atom Stereocenter Count
1
Defined Bond Stereocenter Count
0
Undefined Bond Stereocenter Count
0
The total count of all stereochemical bonds
0
Covalently-Bonded Unit Count
1
Calcolatori di soluzioni
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Recensioni
Recensioni dei clienti
Application Protocols
No tested applications or protocol recommendations are provided for MD-224 in the product data.
Item-specific application guidance:
Not specified for this item; refer to CoA/Spec Sheet.
General protocols for small-molecule use in assays (not item-specific):
Stock preparation:
Weigh accurately, dissolve in anhydrous DMSO to 10–50 mM, vortex, and, if needed, sonicate gently. Filter (0.22 µm PTFE) for sterile applications.
Aliquot and store at −20 °C to avoid repeated freeze–thaw.
Dose–response setup:
Prepare serial dilutions in DMSO, then back-dilute into assay buffer to maintain constant final DMSO across wells (e.g., 0.1–0.5% v/v).
Controls:
Include vehicle control (matching DMSO), positive control compound (assay-dependent), and, if available, an inactive analog.
Stability checks:
Verify concentration by UV or LC where possible; re-check after the assay window to confirm no precipitation/degradation.
Data integrity:
Use replicate wells, randomized plate layouts, and plate maps; monitor edge effects and solvent artifacts.
For any specialized application (e.g., pulldown chemistry, PROTAC assays, photo-crosslinking), obtain the exact structural information and recommended handling from the CoA/Tech Sheet.
Biological Roles
Item-specific biological target, mechanism of action, and pathway engagement for MD-224 are not provided in the product data. Do not infer pharmacology without verified documentation.
Target(s): Not specified for this item; refer to CoA/Spec Sheet or peer-reviewed literature explicitly matching CAS 2136247-12-4.
Mode of action: Not specified for this item; refer to CoA/Spec Sheet.
Pathways/bioprocesses: Not specified for this item; refer to CoA/Spec Sheet.
General guidance for using small molecules in biological experiments (not item-specific):
Confirm identity and purity (HPLC area %, HRMS) prior to biological testing.
Establish solubility and stability in relevant matrices (assay buffer, cell culture media with/without serum). Assess precipitation visually and by LC at working concentrations.
Determine non-specific binding and adsorption (plasticware, serum proteins) via recovery experiments.
Include proper controls: vehicle-only, inactive analogs (if available), and positive controls. Perform concentration–response analyses with adequate replicates and pre-registered data handling.
Phototoxicity/auto-fluorescence: Evaluate optical interference if readouts are absorbance- or fluorescence-based.
Research use only: As stated by the manufacturer, MD-224 is for research use only and is not intended for diagnostic, therapeutic, or other clinical applications.
Buffer Applications
This product is a small-molecule research compound rather than a buffering agent. No specific buffer system or buffering capacity is applicable to MD-224.
Practical notes for preparing assay buffers with small-molecule stocks (general guidance):
Prepare a concentrated DMSO stock and dilute into pre-made buffers (e.g., PBS, HEPES, Tris) to the desired final concentration, keeping DMSO at a constant percentage across all wells/samples.
Typical pH ranges (literature/general):
PBS: pH ~7.2–7.4
HEPES: pH range ~6.8–8.2
Tris: pH range ~7.0–9.0
To minimize precipitation on dilution, add the DMSO stock slowly under vigorous mixing. For poorly soluble compounds, incorporate co-solvents or carriers (e.g., 0.01–0.1% nonionic surfactant) if compatible with the assay.
Item-specific buffer recommendations, pKa, or ionic interactions: Not specified for this item; refer to CoA/Spec Sheet if specialized formulation guidance is provided.
Green Alternatives
Because MD-224 is sold as a small-molecule research compound rather than a bulk solvent or reagent, substitution with a “green alternative” is generally not applicable. However, greener practices can be applied to its handling and use.
Solvent minimization: Use high-concentration DMSO stocks and low final organic solvent percentages in assays (e.g., ≤0.5–1% v/v) to reduce solvent consumption.
Greener solvent choices for analytics: Prefer water-rich mobile phases with acetonitrile over methanol when appropriate for LC separations to reduce energy use in drying; consider supercritical fluid chromatography (SFC) when feasible.
Waste reduction: Plan assays to minimize excess dilutions. Consolidate compatible organic waste streams. Use microplate formats to reduce volume.
Energy-efficient storage: Store only necessary aliquots at −20 °C; retain working aliquots at 4 °C when stability data permit (not specified here—verify first) to reduce freezer door-open time and freeze–thaw cycles.
Packaging and transport: Maintain cold chain as specified (ice chest + ice pads) to avoid re-shipment due to degradation.
Comparison note:
For reagents like extraction solvents or reaction media, greener alternatives can often be proposed (e.g., 2-MeTHF vs THF). For a discrete bioactive compound, substitution is not meaningful; focus on process greening around its use.
Pharmaceutical Uses
No pharmacopeial grade, excipient role, or manufacturing/formulation status is provided for MD-224. This product is designated for research use only and is not for human or veterinary use.
Pharmacopeial listings: Not specified for this item; refer to CoA/Spec Sheet.
Excipient/functionality category: Not specified for this item.
Residual solvent or impurity limits to pharmacopoeial standards: Not specified for this item.
General considerations for preclinical formulation research with small molecules (not item-specific and non-clinical):
Solubilization strategies: co-solvent systems (e.g., PEG400/ethanol/saline), cyclodextrin inclusion complexes (HP-β-CD), lipid-based vehicles, or nanosuspensions. Validate stability and compatibility.
Parenteral vs. enteral vehicles: select based on target route in preclinical models; control pH, osmolality, and excipient safety for the test system. These considerations are presented for general research planning only.
Compliance note:
Do not use this product in drug substances, drug products, or clinical studies without appropriate qualification and regulatory review. For any translational work, source GMP-grade material and full CMC data; this catalog item is not supplied as GMP.
Physical Properties
Only item-specific properties listed below are definitive. All other values are “Not specified” here and should be verified on the Certificate of Analysis (CoA) for the shipped lot.
Appearance: Not specified for this item; refer to CoA/Spec Sheet.
Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
Molecular formula: 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 specified for this item; refer to CoA/Spec Sheet.
Density: Not specified for this item; refer to CoA/Spec Sheet.
Refractive index: Not applicable/not specified for solid materials; refer to CoA/Spec Sheet if provided.
Solubility: Not specified for this item; refer to CoA/Spec Sheet. (General practice for small-molecule screening compounds is to prepare concentrated DMSO stocks and dilute into aqueous buffers with co-solvent.)
pKa/logP/logD: Not specified for this item; refer to CoA/Spec Sheet.
UV-Vis characteristics: Not specified for this item; refer to CoA/Spec Sheet.
General considerations for unknown/unspecified small molecules (literature/guidance, not item-specific):
Many drug-like molecules dissolve well in anhydrous DMSO (10–50 mg/mL) and variably in methanol/acetonitrile; aqueous solubility is often formulation-dependent (cosolvent, surfactant, or cyclodextrin). Optimize empirically.
If photolabile chromophores are suspected, protect from light during handling and storage.
Quality and Grades
Grade/purity information is not specified in the provided product data and should be confirmed on the CoA/Spec Sheet for your specific lot. The following guidance explains typical grading and documentation for small-molecule research compounds.
Grade/purity (item-specific): Not specified for this item; refer to CoA/Spec Sheet.
Stabilizers/inhibitors: Not specified for this item; refer to CoA/Spec Sheet. If present, stabilizers will be listed and may affect analytical baselines (e.g., UV background) and bioassays.
Typical quality documentation (general):
Identity confirmation by NMR and/or HRMS.
Purity by HPLC/UPLC (area %) with chromatogram and method details.
Water and residual solvent content by Karl Fischer and GC, respectively (where applicable).
Inorganic residue/metals (ICP) if relevant to application.
What the grade means (general): For screening compounds, “research grade” typically denotes suitability for discovery research use, not meeting pharmacopeial monographs. HPLC-grade solvents pertain to solvents only and are not relevant here; for solids, reported purity is customarily area % by HPLC.
Batch-to-batch consistency: Verify that the batch number on the label matches the CoA. For critical applications (biophysical assays, crystallography), consider internal re-qualification (e.g., orthogonal purity metrics, counterion analysis) before use.
Reaction and Applications
This catalog entry is classified under “Small Molecules and Compound Libraries,” and is intended primarily as a research tool compound rather than a synthetic reagent. No specific reactivity, catalytic role, or application claims are provided for MD-224 in the product data.
Item-specific applications:
Not specified for this item; refer to CoA/Spec Sheet or associated technical notes.
General research uses for small molecules (guidance, not item-specific claims):
Screening and profiling: evaluation in biochemical/biophysical assays, cellular phenotypic screens, or target engagement studies.
Mechanistic studies: use as a chemical probe when the target and mode of action are known (consult literature/CoA before assigning mechanism).
Analytical reference: potential use as a reference standard in method development/validation once structural identity and purity are confirmed.
Practical tips:
Prepare concentrated DMSO stocks to minimize freeze–thaw cycles; aliquot upon first thaw.
Verify stability under assay conditions (temperature, pH, light). Conduct small-scale pretests to assess adsorption to plastics and serum protein binding where relevant.
If the compound is chromophoric or fluorescent (unknown here), account for optical interference in readouts (absorbance/fluorescence), and include solvent-only controls.
Synthesis-related applications:
Without a disclosed structure, guidance for use in named reactions or as a building block is not applicable. If you intend to use MD-224 as a synthetic intermediate, request full structural documentation first.
Reaction Conditions
No reaction conditions are specified for MD-224, and it is not presented as a reagent or catalyst. Therefore, reaction parameters (solvents, catalysts, temperatures, times, yields) are not applicable to this listing.
General guidance (not item-specific) if using a small molecule of unknown reactivity in chemical transformations:
Conduct a small-scale feasibility test while monitoring by LC-MS/UPLC to detect degradation or unintended reactions.
Screen mild conditions first (neutral pH, room temperature, oxygen exclusion if needed). Avoid strong acids/bases and strong oxidants/reductants until compatibility is known.
Use inert atmosphere and anhydrous solvents for moisture-sensitive functionalities if suspected.
Purification: Prefer reverse-phase chromatography for polar/ionizable molecules; normal-phase silica may induce decomposition for acid-/base-labile compounds.
For this catalog item as supplied, prioritize applications as a research tool compound rather than as a reagent in synthetic chemistry.
Safety and Handling
Authoritative safety information must be taken from the product’s SDS. The following fields are not specified in the provided data and must be confirmed on the SDS/CoA:
GHS classification: Not specified for this item; refer to SDS.
Signal word: Not specified for this item; refer to SDS.
Hazard statements (H-phrases): Not specified for this item; refer to SDS.
Pictograms: Not specified for this item; refer to SDS.
General laboratory precautions for small organic research compounds (guidance, not item-specific):
PPE: Wear lab coat, suitable gloves (e.g., nitrile), safety glasses or face shield when splashing risk exists. Handle powders in a fume hood to avoid inhalation and dust exposure.
Avoid ingestion, inhalation, and skin/eye contact. Use local exhaust ventilation. Prevent environmental release.
Incompatibilities: Until structure is known, avoid strong oxidizers/reductants, strong acids/bases, and conditions that could decompose unknown functional groups. Segregate from foodstuffs and incompatible chemicals.
First aid (overview): If on skin/eyes, rinse with water for 15 minutes; remove contaminated clothing. If inhaled, move to fresh air. If ingested, rinse mouth; seek medical attention. Always follow institutional EHS protocols and SDS guidance.
Spill response: For small spills, absorb with inert material and collect as hazardous waste. Avoid dust generation. For large spills, evacuate area and consult EHS.
Special risks: Not specified for this item. If the compound is moisture-, air-, or light-sensitive, handle under inert gas and protect from light as appropriate; consult CoA/SDS.
Solvent Selection
Item-specific solubility is not provided. The following is practical guidance for dissolving small-molecule research compounds with unknown solubility profiles.
Primary stock solvent (general best practice):
Anhydrous DMSO is the default for many drug-like molecules; aim for 10–50 mM master stocks when feasible. Filter-sterilize (0.22 µm PTFE) if needed for cell-based work.
Co-solvent systems for assay buffers:
Aqueous buffers with 0.1–1% DMSO are typical for biochemical assays; up to 0.5–1% (v/v) DMSO is often tolerated in mammalian cell culture. Validate tolerance empirically.
Alternative organic vehicles: methanol or acetonitrile for LC workflows; ethanol for some biological assays. Introduce organic solvent slowly under vortex to avoid precipitation.
Polarity and miscibility (general): DMSO is polar aprotic and fully miscible with water; methanol and acetonitrile are also miscible. For hydrophobic compounds, consider co-solvents plus surfactants (0.01–0.1% Tween-80) or complexation (e.g., 2–10% (w/v) HP-β-CD) as assay-appropriate.
Troubleshooting precipitation:
Sonication and gentle warming (≤37 °C) can help dissolution. Avoid repeated heating/cooling cycles which may degrade sensitive compounds.
Compatibility notes:
Avoid strong acids/bases unless stability is established. For LC-MS, prefer LC-MS-grade solvents and minimize nonvolatile buffers.
Storage and Reconstitution
Item-specific storage and shipping conditions are provided below, taken directly from the product data. Additional reconstitution guidance is general and should be adapted once structure/solubility are known.
Storage conditions (item-specific): Store at −20 °C.
Shipped in (item-specific): Ice chest + Ice pads.
Appearance (item-specific): Not specified for this item; refer to CoA/Spec Sheet.
Reconstitution (general guidance for small molecules; not item-specific specifications):
Solvent choice: Start with anhydrous DMSO for master stocks unless contraindicated by the CoA.
Concentration: Common stock levels are 10–50 mM; adjust based on observed solubility and assay needs. If solubility is limited, consider 1–5 mM stocks or use co-solvents.
Technique: Allow vial to equilibrate to room temperature before opening to minimize condensation. Weigh quickly, cap promptly, and purge with inert gas if moisture- or air-sensitive behavior is suspected.
Aliquoting: Prepare single-use aliquots to avoid repeated freeze–thaw. Label with compound ID, lot, concentration, solvent, and date.
Short-term handling: Keep working solutions on ice or at 4 °C during use if stability is uncertain; protect from light when in doubt.
Stability/shelf life (item-specific): Not specified for this item; refer to CoA/Spec Sheet. Always defer to the SDS/CoA for authoritative guidance.
Structure and Identity
Item-specific identifiers provided for this catalog entry are limited. Where values are not provided, consult the CoA/Spec Sheet for the specific lot.
Item name: MD-224 (SKU: M649182)
CAS: 2136247-12-4
CID: 131986956
InChIKey: 460043 (as provided; truncated/atypical formatting — verify against 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 guidance):
Structural class: Not specified for this item. MD-224 is listed under “Small Molecules and Compound Libraries,” indicating a research screening compound. Without a structure, ring systems, substituent patterns, and stereochemistry cannot be described.
2D structure (descriptive):
Not available in the product data. If you require an annotated 2D depiction, request the structure file (SDF/MOL) from the CoA or supporting documentation.
Notes for identity confirmation (general best practices):
Verify identity by orthogonal methods when the structure is known (e.g., HRMS, 1H/13C NMR, and HPLC/UPLC purity profile).
Cross-check CAS and any public registry links (e.g., PubChem CID) against the supplied batch documentation to ensure congruence with the shipped material.
Synthetic Utility
MD-224 is supplied as a research small molecule intended for biological/assay use. Without a disclosed structure, it is not possible to describe functional groups, synthetic handles, or expected reactivity.
Item-specific synthetic roles:
Not specified for this item; refer to CoA/Spec Sheet if a structure is disclosed.
General considerations (not item-specific):
If the structure becomes available and you intend to use the compound as a building block or reference material, assess:
Functional group compatibility (acid/base sensitivity, oxidation state, protecting group strategy).
Stability under common workup conditions (aqueous acid/base, peroxide-prone solvents, silica exposure).
Scalability and purification routes (normal-phase vs reverse-phase chromatography, crystallization feasibility).
Reference standards: Compounds with confirmed structure and purity can serve as analytical standards for LC/GC method development, provided they are stable and well-characterized.
Until the structural identity and reactivity are documented, treat MD-224 as a finished small-molecule probe rather than a synthetic intermediate.
Target Specificity
Target, selectivity profile, and off-target data for MD-224 are not provided in the product data.
Primary target: Not specified for this item; refer to CoA/Spec Sheet or peer-reviewed literature tied explicitly to CAS 2136247-12-4.
Secondary/off-targets: Not specified for this item; refer to CoA/Spec Sheet.
Species reactivity: Not specified for this item; refer to CoA/Spec Sheet.
Assay context: Not specified for this item; refer to CoA/Spec Sheet.
Guidance for establishing target specificity (general, not item-specific):
Combine biochemical potency assays with cellular target-engagement (e.g., CETSA, NanoBRET) and orthogonal phenotypic readouts.
Use counter-screens against related family members and broad profiling panels (kinome, receptor binding, etc.) as appropriate.
Quantify selectivity indices and incorporate genetic controls (knockout/knockdown or overexpression) to link phenotype to target modulation.
Please consult the SDS and CoA for any item-specific claims or data that accompany your shipped lot.
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