| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
This compound is a chemical linker rather than a drug with a specific biological target. It serves as a conjugation tool for attaching payloads to antibodies or other proteins, with enhanced stability compared to NHS ester-based linkers.
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|---|---|
| ln Vitro |
Mal-PEG4-PFP ester does not possess intrinsic biological activity. Its utility is demonstrated through conjugation reactions: the PFP ester reacts with lysine amines on proteins under mild aqueous conditions (pH 7.0-8.0) to form amide bonds, while the maleimide reacts with cysteine thiols (pH 6.5-7.5) to form stable thioether bonds.
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| ln Vivo |
This compound is not designed for direct in vivo administration. Its in vivo relevance is demonstrated through the efficacy of ADCs synthesized using this linker. The PFP ester provides improved stability in aqueous environments compared to NHS esters, enabling more efficient conjugations.
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| Enzyme Assay |
Conjugation efficiency is assessed by HPLC, LC-MS, or MALDI-TOF. PFP ester reactions with amines are performed at pH 7.0-8.0 in PBS or HEPES buffer. Maleimide-thiol reactions are conducted at pH 6.5-7.5. The degree of conjugation is determined by UV-Vis or mass spectrometry. PFP ester stability is monitored by HPLC.
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| Cell Assay |
No cell-based assays are performed for the linker itself. Cell-based assays are conducted with the final ADC conjugate. These include cell viability assays on target antigen-expressing cancer cell lines, receptor binding assays, and internalization studies.
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| Animal Protocol |
In vivo efficacy studies are performed with the final ADC conjugate in mouse xenograft models. Tumor-bearing mice are treated with the conjugate via intravenous administration. Tumor growth inhibition, body weight, and survival are monitored. Pharmacokinetic studies assess conjugate stability and payload release.
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| ADME/Pharmacokinetics |
Mal-PEG4-PFP has molecular weight approximately 497.4 and formula C20H22F5NO7. It is soluble in DMSO, DMF, and acetonitrile. The PFP ester is more hydrolytically stable than NHS esters. The PEG4 spacer provides good hydrophilicity. The compound should be stored desiccated at -20°C.
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| Toxicity/Toxicokinetics |
As a chemical linker rather than a therapeutic agent, Mal-PEG4-PFP has no intrinsic toxicity. Toxicity is assessed at the level of the final ADC conjugate. The PFP ester is hydrolyzed during conjugation. Standard toxicological assessments are performed with the complete conjugate.
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| Additional Infomation |
Mal-PEG4-PFP is a research-grade PEG linker used for bioconjugation applications. The PFP ester provides enhanced stability for aqueous conjugation reactions compared to NHS esters. This linker is employed in ADC synthesis where controlled, efficient conjugation is required. No clinical trials or approved therapeutic applications exist.
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| Molecular Formula |
C21H22F5NO8
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|---|---|
| Molecular Weight |
511.393304347992
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| Exact Mass |
453.084
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| CAS # |
1415800-42-8
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| PubChem CID |
77078506
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| Appearance |
Off-white to light brown viscous liquid
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
516.1±50.0 °C at 760 mmHg
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| Flash Point |
265.9±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.499
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| LogP |
1.78
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
35
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| Complexity |
696
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C(=C(C(=C(C=1OC(CCOCCOCCOCCOCCN1C(C=CC1=O)=O)=O)F)F)F)F
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| InChi Key |
XGSVXFAIAZKWST-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22F5NO8/c22-16-17(23)19(25)21(20(26)18(16)24)35-15(30)3-5-31-7-9-33-11-12-34-10-8-32-6-4-27-13(28)1-2-14(27)29/h1-2H,3-12H2
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| Chemical Name |
(2,3,4,5,6-pentafluorophenyl) 3-[2-[2-[2-[2-(2,5-dioxopyrrol-1-yl)ethoxy]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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9555 mL | 9.7773 mL | 19.5545 mL | |
| 5 mM | 0.3911 mL | 1.9555 mL | 3.9109 mL | |
| 10 mM | 0.1955 mL | 0.9777 mL | 1.9555 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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