| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Not applicable. NHPI-PEG4-C2-Pfp ester is a non-cleavable PEG linker used in ADC synthesis, not a drug. It has no biological target. The NHPI (N-hydroxyphthalimide) ester is an activated ester that can react with amine groups. The Pfp (pentafluorophenyl) ester is an excellent leaving group for efficient acylation reactions. The PEG4 spacer (four ethylene glycol units) provides water solubility and reduces non-specific protein binding. As a non-cleavable linker, the final ADC is not cleaved in the lysosome; instead, the entire antibody is degraded and the payload is released.
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|---|---|
| ln Vitro |
No significant direct in vitro activity is reported. As a chemical linker, NHPI-PEG4-C2-Pfp ester is used to conjugate cytotoxic payloads (e.g., auristatins, maytansinoids) to antibodies. The resulting ADCs exhibit potent in vitro cytotoxicity against target-positive cancer cells. The PEG4 spacer ensures solubility and prevents aggregation of the ADC. The purity is typically ≥95%.
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| ln Vivo |
No specific in vivo data is reported. ADCs synthesized with this non-cleavable PEG4 linker exhibit good in vivo stability and efficacy in tumor xenograft models. Non-cleavable linkers can provide a wider therapeutic window by reducing off-target toxicity because the payload is not released until the entire antibody is degraded inside the target cell. The PEG4 spacer contributes to favorable pharmacokinetic properties.
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| Enzyme Assay |
Not applicable. NHPI-PEG4-C2-Pfp ester is a chemical reagent used for bioconjugation. A typical conjugation protocol involves dissolving the linker (1-10 mM) in anhydrous DMSO or DMF. To conjugate an amine-containing payload (e.g., a cytotoxic drug with a free amine), the linker and payload are reacted in a 1:1.2 molar ratio in the presence of a base (e.g., DIPEA) at room temperature for 2-6 hours. The resulting NHPI-PEG4-C2-Pfp-payload conjugate is purified by HPLC. This intermediate can then be conjugated to an antibody via NHS ester chemistry or other reactive groups.
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| Cell Assay |
Not applicable. The compound itself is not used in cell-based assays. The final ADC produced with this linker is tested in vitro. Target-positive and target-negative cancer cells are seeded in 96-well plates (5,000 cells/well) and treated with serial dilutions of the ADC for 72-96 hours. Cell viability is assessed by CellTiter-Glo. The selectivity index (IC50 ratio between target-negative and target-positive cells) is calculated. Non-cleavable ADCs typically exhibit less bystander killing effect but have a more predictable safety profile.
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| Animal Protocol |
No specific in vivo animal study protocols are documented. For an ADC synthesized with this non-cleavable PEG4 linker, a typical protocol involves intravenous administration of the ADC (1-10 mg/kg) in tumor xenograft models in mice. Efficacy is assessed by tumor growth inhibition. The non-cleavable linker is expected to be stable in circulation for an extended period (days), with the intact ADC as the predominant circulating species. Biodistribution studies measure ADC concentration in tumor and normal tissues.
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| ADME/Pharmacokinetics |
Not applicable for the linker. The PEG4 spacer imparts favorable PK properties to the final ADC. PEGylation reduces renal clearance and increases the circulation half-life of the conjugated product. The non-cleavable nature ensures that the ADC is cleared as the intact conjugate, minimizing premature payload release. The half-life is primarily determined by the antibody scaffold (typically 7-14 days in mice).
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| Toxicity/Toxicokinetics |
No toxicity data is reported for NHPI-PEG4-C2-Pfp ester. As a chemical reagent, standard safety precautions apply. The Pfp (pentafluorophenyl) ester is reactive and may be an irritant. The final ADC payload is highly potent and should be handled in a designated biosafety cabinet. The compound is for research use only.
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| Additional Infomation |
NHPI-PEG4-C2-Pfp ester has the molecular formula C25H24F5NO9 and a molecular weight of 577.45. The IUPAC name is (2,3,4,5,6-pentafluorophenyl) 3-[2-[2-[2-[2-(1,3-dioxoisoindol-2-yl)oxyethoxy]ethoxy]ethoxy]ethoxy]propanoate. It is a pale yellow or colorless oil that is soluble in DMSO. The compound is stored at 2-8degC and is stable for long-term storage. It is used exclusively for ADC research and development.
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| Molecular Formula |
C25H24F5NO9
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|---|---|
| Exact Mass |
577.137
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| CAS # |
2101206-46-4
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| PubChem CID |
129896963
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| Appearance |
Colorless to light yellow liquid（Density：1.45 g/cm3）
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
40
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| Complexity |
788
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C(=O)N(C2=O)OCCOCCOCCOCCOCCC(=O)OC3=C(C(=C(C(=C3F)F)F)F)F
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| InChi Key |
XHCPQOPVDGGVBJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24F5NO9/c26-18-19(27)21(29)23(22(30)20(18)28)40-17(32)5-6-35-7-8-36-9-10-37-11-12-38-13-14-39-31-24(33)15-3-1-2-4-16(15)25(31)34/h1-4H,5-14H2
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| Chemical Name |
(2,3,4,5,6-pentafluorophenyl) 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.
Products are for research use only; We do not sell to patients
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