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Iodo-PEG7-alcohol

Cat No.:V76886 Purity: ≥98%
Iodo-PEG7-alcohol is a PROTAC (PROteolysis TArgeting Chimera) linker, which belongs to the Polyethylene glycol (PEG) category and may be utilized to prepare PROTAC protein degraders.
Iodo-PEG7-alcohol
Iodo-PEG7-alcohol Chemical Structure Product category: PROTAC Linkers
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
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Product Description
Iodo-PEG7-alcohol is a PROTAC (PROteolysis TArgeting Chimera) linker, which belongs to the Polyethylene glycol (PEG) category and may be utilized to prepare PROTAC protein degraders.
Iodo-PEG7-alcohol is a polyethylene glycol (PEG)-based linker compound containing an iodine atom at one end and a hydroxyl group at the other end, with seven PEG units. It is used as a building block for antibody-drug conjugates (ADCs) and PROTACs, enabling the attachment of payloads to targeting moieties via alkylation or substitution reactions.
Biological Activity I Assay Protocols (From Reference)
Targets
PEGs
Iodo-PEG7-alcohol does not target a specific biological receptor; it is a chemical linker. The iodo group serves as a leaving group in nucleophilic substitution reactions (SN2) with thiols, amines, or other nucleophiles. The alcohol group can be further functionalized (e.g., activated as a carbonate or succinimidyl ester) for conjugation to proteins or small molecules.
ln Vitro
A linker separates the two ligands that make up PROTACs; one ligand is for an E3 ubiquitin ligase, and the other is for the target protein. Target proteins are selectively degraded by PROTACs by taking advantage of the intracellular ubiquitin-proteasome system[1].
Iodo-PEG7-alcohol is not used in enzyme/receptor binding assays. Its reactivity is evaluated in cell-free chemical reactions. For example, it reacts with thiol-containing compounds (e.g., cysteine, glutathione) in aqueous buffer at pH 7-9 to form a stable thioether linkage. Reaction progress is monitored by HPLC or LC-MS. No biological activity is intended or observed.
ln Vivo
In cell culture, Iodo-PEG7-alcohol (typically 1-100 uM) can be used to label surface-exposed thiols on proteins if the iodo group is reactive. However, it is generally not used directly on cells; instead, it is first conjugated to a targeting ligand (e.g., antibody) via the alcohol group after activation. The conjugate then binds to the target cell. The compound itself has no inherent cytotoxicity at working concentrations.
Enzyme Assay
To test reactivity, a cell-free assay is performed: Iodo-PEG7-alcohol (10-100 uM) is incubated with a thiol-containing model compound (e.g., N-acetylcysteine, 1 mM) in PBS (pH 7.4) at 37degC for 1-24 hours. Aliquots are taken and analyzed by HPLC or LC-MS to determine the conversion rate. The reaction is typically complete within a few hours. Control reactions without thiol show no change. The reaction follows second-order kinetics.
Cell Assay
If Iodo-PEG7-alcohol is conjugated to a cell-targeting ligand (e.g., an RGD peptide), the conjugate is incubated with target cells (e.g., integrin-expressing cancer cells) at 1-10 uM for 1-4 hours. Cellular binding is assessed by flow cytometry using a fluorescent tag attached via the alcohol group (after activation). Alternatively, the conjugate can deliver a payload (e.g., drug) to cells, and cytotoxicity is measured by MTT. The PEG7 spacer enhances solubility and reduces steric hindrance.
Animal Protocol
Iodo-PEG7-alcohol itself is rarely administered in vivo. Instead, it is used ex vivo to synthesize conjugates that are then administered. For example, an ADC made using this linker is given intravenously in tumor-bearing mice at 1-10 mg/kg. The linker is stable in circulation; the iodine atom is displaced only upon intracellular thiol exposure. The alcohol end can be used for further conjugation. PK studies are performed on the final conjugate, not the linker alone.
ADME/Pharmacokinetics
As a small PEGylated molecule, Iodo-PEG7-alcohol has a molecular weight of approximately 450-500 Da. It is soluble in water and common organic solvents (DMSO, DMF). The iodo group is reactive and may undergo hydrolysis at high pH or in the presence of light. The compound should be stored at -20degC under inert atmosphere, protected from light. The PEG7 chain imparts hydrophilicity and reduces non-specific protein binding.
Toxicity/Toxicokinetics
Iodo-PEG7-alcohol is considered a chemical reagent with low acute toxicity. The iodo group can be alkylating, so the compound should be handled with care (potential skin/eye irritant). In cellular assays at ≤100 uM, no significant cytotoxicity has been reported. For in vivo use of conjugates, the linker itself is typically non-toxic at the doses delivered. Standard lab safety (gloves, goggles, fume hood) is recommended.
References
[1]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
Additional Infomation
Iodo-PEG7-alcohol is a research chemical used as a linker in the synthesis of ADCs, PROTACs, and other bioconjugates. The PEG7 spacer provides a hydrophilic, flexible bridge that improves solubility and reduces aggregation. The iodine atom is an excellent leaving group for thiol-alkylation. The alcohol group can be converted to an active ester (NHS) or other functional groups. This product is for laboratory use only and is not approved for human therapeutic use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H29IO7
Molecular Weight
436.28
Appearance
Colorless to light yellow liquid
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2921 mL 11.4605 mL 22.9211 mL
5 mM 0.4584 mL 2.2921 mL 4.5842 mL
10 mM 0.2292 mL 1.1461 mL 2.2921 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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