| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
As a chemical linker for ADC construction, NHPI-PEG4-C2-NHS ester does not have a defined biological target. Its role is to serve as a cleavable connector between an antibody and a cytotoxic payload in antibody-drug conjugates. The NHPI moiety provides a cleavable site that enables controlled release of the drug payload under specific conditions. The PEG4 spacer enhances solubility and biocompatibility, facilitating the delivery of the ADC to target cells.
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| ln Vitro |
In cell-free biochemical systems, this linker is used to covalently attach small molecule drugs to antibodies, enabling the formation of stable antibody-drug conjugates. The NHS ester reacts with primary amines on the antibody, while the NHPI group provides a cleavable linkage for drug release. The PEG4 spacer improves the solubility and stability of the resulting conjugate in aqueous environments. The linker facilitates the synthesis of ADCs with controlled drug-to-antibody ratios.
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| ln Vivo |
For antibody drug conjugates (ADCs), NHPI-PEG4-C2-NHS ester, Example 40 (WO2014185985.A1), can serve as a connecting link.
This compound does not exhibit direct cellular activity as it is a chemical linker rather than a bioactive molecule. Antibody-drug conjugates constructed using this linker can be delivered to target cells where the antibody binds to cell surface antigens, followed by internalization and intracellular release of the cytotoxic payload. The cleavable nature of the NHPI group enables controlled drug release within target cells. |
| Enzyme Assay |
The cell-free assay for this linker involves conjugation reactions between the NHS ester and primary amines on proteins or antibodies. The reaction is typically performed in aqueous buffer at pH 7.4-8.5 for 1-4 hours at room temperature or 4°C. The efficiency of conjugation is assessed by mass spectrometry, SDS-PAGE, or HPLC analysis. The purity and integrity of the resulting conjugate are evaluated to confirm successful linker incorporation.
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| Cell Assay |
No cell-based experimental protocols are directly applicable to this linker as it is a chemical synthesis reagent. Antibody-drug conjugates synthesized using this linker can be evaluated in cell culture experiments. Typical protocols include treating cancer cell lines expressing the target antigen with the ADC at concentrations ranging from 0.001 to 10 μg/mL. Cells are incubated for 24-96 hours, and cell viability is assessed using MTT or CCK-8 assays. The specificity of target cell killing is evaluated by comparing antigen-positive and antigen-negative cell lines.
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| Animal Protocol |
This linker is not administered to animals as it is a chemical intermediate for ADC synthesis. Antibody-drug conjugates incorporating this linker may be evaluated in animal models for pharmacokinetics and efficacy. Typical studies involve administration of the ADC to tumor-bearing mice via intravenous routes at doses ranging from 0.1-10 mg/kg. Tumor volumes are measured, and tissues are collected for analysis of ADC distribution, payload release, and therapeutic efficacy.
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| ADME/Pharmacokinetics |
As a chemical reagent, this compound does not have established pharmacokinetic properties. The pharmacokinetics of ADCs incorporating this linker depend on the antibody, payload, and overall conjugate properties. The cleavable nature of the NHPI group influences payload release kinetics. The PEG4 spacer may affect the circulation time and biodistribution of the ADC. The compound itself is not intended for therapeutic use and is not administered systemically.
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| Toxicity/Toxicokinetics |
The compound is not intended for therapeutic use and lacks established toxicity profiles. Standard laboratory safety precautions should be observed when handling this chemical reagent. The compound is typically stored at 2-8°C. As an NHS ester, it is moisture-sensitive and should be handled under anhydrous conditions. The compound is for research use only and is not for human or veterinary therapeutic applications.
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| References |
[1]. Shailaja SRINAGESH, et al. Novel polypeptide small molecule conjugates and their uses
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| Additional Infomation |
NHPI-PEG4-C2-NHS ester is a research-grade chemical supplied for ADC linker synthesis applications. It is not an approved pharmaceutical and has no clinical trial history. The compound is also known as example 40 from WO2014185985A1. Purity specifications generally exceed 98%. Appearance is typically a pale yellow or colorless oily matter. The compound is soluble in DMSO. This product is intended for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C23H28N2O11
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|---|---|
| Exact Mass |
508.169
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| CAS # |
1415328-95-8
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| PubChem CID |
89284647
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| Appearance |
Colorless to light yellow viscous liquid
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| LogP |
-0.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
36
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| Complexity |
750
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(=O)N(C1=O)OC(=O)CCOCCOCCOCCOCCON2C(=O)C3=CC=CC=C3C2=O
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| InChi Key |
HLAGLPXQSIDIDX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H28N2O11/c26-19-5-6-20(27)24(19)36-21(28)7-8-31-9-10-32-11-12-33-13-14-34-15-16-35-25-22(29)17-3-1-2-4-18(17)23(25)30/h1-4H,5-16H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 3-[2-[2-[2-[2-(1,3-dioxoisoindol-2-yl)oxyethoxy]ethoxy]ethoxy]ethoxy]propanoate
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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.) |
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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