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| Other Sizes |
| Targets |
Hydroxy-PEG1-acid does not have a specific biological target, as it is a chemical linker. Its function is to serve as a covalent connector between two or more molecular components in the synthesis of ADCs. The terminal carboxyl group is a target for conjugation with molecules that contain primary amines, forming a stable amide bond. The hydroxyl group can be used for further functionalization. The short PEG1 spacer enhances solubility and reduces steric hindrance. In the context of ADC design, the linker's role is to connect the cytotoxic payload to the targeting antibody, ensuring stability in circulation and efficient release of the payload at the target site.
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| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1].
As a chemical linker, Hydroxy-PEG1-acid does not possess any direct in vitro biological activity. Its function is to serve as a covalent bridge in the synthesis of ADCs. The in vitro activity of this linker is assessed indirectly through the characterization of the final ADCs it helps to create. For instance, the activity of the ADC is evaluated in cell-based assays for target binding, internalization, and cytotoxicity. The linker contributes to the ADC's overall activity by ensuring stable attachment and proper release of the payload. Thus, the activity of Hydroxy-PEG1-acid is a measure of its utility as a synthetic building block. |
| ln Vivo |
As a chemical linker, Hydroxy-PEG1-acid does not possess any direct in vivo biological activity. It is not administered as a therapeutic agent and does not exert pharmacological effects in animal models. Its in vivo relevance is strictly as a component of larger, biologically active ADCs. When incorporated into an ADC, the non-cleavable linker ensures stable attachment of the payload to the antibody. The specific in vivo activity—such as tumor regression—is determined by the ADC's warhead and targeting ligand, not the linker itself. The linker's role is permissive, ensuring that the active components are stably connected.
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| Enzyme Assay |
There are no specific in vitro enzyme or receptor binding assays for Hydroxy-PEG1-acid, as it is not a biologically active compound. The compound is a chemical reagent, and its characterization is performed using analytical chemistry techniques. The quality and identity of the linker are typically confirmed by methods such as NMR, HPLC, and MS to verify its structure and purity. The reactivity of the carboxyl group can be tested by reacting the compound with a model amine and monitoring the formation of the amide bond. These are quality control steps, not biological assays.
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| Cell Assay |
There are no standard in vitro cell-based assays for Hydroxy-PEG1-acid, as it is not a bioactive molecule. Its use in cell biology is indirect, as a reagent for constructing ADCs. In such cases, the cell-based assay would involve treating cells with the final ADC and then measuring a biological readout, such as cell viability. The performance of the linker would be evaluated by the potency and selectivity of the ADC, which depend on the linker's ability to connect the components effectively. However, there is no direct assay for the linker itself in cells.
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| Animal Protocol |
Hydroxy-PEG1-acid is not used in in vivo animal experiments as a standalone compound, as it has no direct biological activity. It is a synthetic building block for creating ADCs. Animal studies involving this compound would only be conducted on the final, larger ADCs that incorporate it. In such studies, the linker's contribution to the overall pharmacokinetic and pharmacodynamic profile of the ADC would be assessed. However, there is no standard animal protocol for the linker itself. Its use is limited to the research and development phase, where it is employed in the chemical synthesis of test articles.
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| ADME/Pharmacokinetics |
Hydroxy-PEG1-acid has a molecular weight of 134.13 g/mol and a molecular formula of C5H10O4. It is a solid compound. For storage, it is recommended to keep the pure form at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. Pharmacokinetic properties are not relevant as the compound is a linker, not a therapeutic agent.
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| Toxicity/Toxicokinetics |
Hydroxy-PEG1-acid is considered to have low toxicity, consistent with other PEG-based linkers. PEG polymers are widely regarded as biocompatible, non-toxic, and non-immunogenic. The compound is classified as a research reagent, and standard laboratory safety precautions should be followed when handling it. Its toxicity profile has not been extensively studied, but due to its intended use and chemical class, it is not expected to be acutely toxic.
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| References |
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
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| Additional Infomation |
Hydroxy-PEG1-acid is a research-use-only reagent and is not a drug, nor is it approved for any clinical or therapeutic use. It is a non-cleavable 1-unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It is a hydrophilic ADC linker intermediate with a short PEG1 spacer and a terminal carboxyl group, enhancing solubility and enabling versatile conjugation. Hydroxy-PEG1-acid can be used to prepare active antibody-drug conjugates (ADCs). It is a valuable tool for medicinal chemists and chemical biologists working on targeted drug delivery and bioconjugation.
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| Molecular Formula |
C5H10O4
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|---|---|
| Molecular Weight |
134.1305
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| Exact Mass |
134.058
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| CAS # |
89211-34-7
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| Related CAS # |
117786-94-4
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| PubChem CID |
21728278
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| Appearance |
Colorless to light yellow liquid（Density：1.224±0.06 g/cm3）
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| LogP |
-1.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
9
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| Complexity |
81
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCOCCO)O
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| InChi Key |
GTIFLSYPOXYYFG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H10O4/c6-2-4-9-3-1-5(7)8/h6H,1-4H2,(H,7,8)
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| Chemical Name |
3-(2-hydroxyethoxy)propanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 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
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 ：Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.4555 mL | 37.2773 mL | 74.5545 mL | |
| 5 mM | 1.4911 mL | 7.4555 mL | 14.9109 mL | |
| 10 mM | 0.7455 mL | 3.7277 mL | 7.4555 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.
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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