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PEG-bis-amine (MW 8000) (Poly(ethylene glycol)-bis-amine (MW 8000))

Cat No.:V73416 Purity: ≥98%
PEG-bis-amine (MW 8000) synthesizes folic acid-conjugated polymer micelles for encapsulation of the anticancer agent 9-nitrocamptothecin.
PEG-bis-amine (MW 8000) (Poly(ethylene glycol)-bis-amine (MW 8000))
PEG-bis-amine (MW 8000) (Poly(ethylene glycol)-bis-amine (MW 8000)) Chemical Structure CAS No.: 24991-53-5
Product category: Liposome
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
1g
Other Sizes
Official Supplier of:
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Product Description
PEG-bis-amine (MW 8000) synthesizes folic acid-conjugated polymer micelles for encapsulation of the anticancer agent 9-nitrocamptothecin. Folic acid-conjugated polymer micelles are effective carriers of poorly soluble anticancer drugs, which can avoid macrophages and function through folate receptor (FR)-mediated endocytosis targeting tumor cells.
PEG-bis-amine (MW 8000), also known as poly(ethylene glycol)-bis-amine, is a linear polyethylene glycol polymer with amine groups (-NH2) at both termini and an average molecular weight of 8000 Da. It is a versatile polymer used in bioconjugation, drug delivery, surface modification, and hydrogel formation due to its excellent biocompatibility, solubility, and ability to form covalent amide bonds with carboxyl groups.
Biological Activity I Assay Protocols (From Reference)
Targets
Not applicable (polymer vehicle/excipient). PEG-bis-amine is a biocompatible polymer that does not have a specific therapeutic target; rather, it is used as a drug delivery carrier, hydrogel scaffold, or surface modifier.
ln Vitro
PEG-bis-amine is not a drug and has no inherent enzyme inhibitory or cell-killing activity. Its "activity" is physicochemical: the terminal amine groups can covalently attach to biomolecules (e.g., proteins, drugs, targeting ligands) via amide bond formation. It enhances solubility, reduces immunogenicity, and prolongs circulation time of conjugated therapeutics.
ln Vivo
PEG-bis-amine has been used in vivo to synthesize folate-conjugated polymer micelles for encapsulating anticancer agents such as 9-nitrocamptothecin. Micelles formed with PEG-bis-amine can target tumors via folate receptor-mediated endocytosis. The polymer itself is inert and biocompatible, making it a safe and effective drug delivery vehicle in animal models.
Enzyme Assay
Cell-free assays for PEG-bis-amine are not typical. However, for bioconjugation: the polymer is dissolved in an appropriate buffer (e.g., MES or PBS, pH 5-7.5). A crosslinker such as EDC/NHS is added to activate the amine groups, and the polymer is then reacted with a carboxyl-group-containing drug or ligand. Conjugation efficiency is analyzed by NMR, MALDI-TOF, or size-exclusion chromatography.
Cell Assay
For cellular assays, cells are treated with drug-loaded PEG-bis-amine micelles or nanoparticles (1-100 microg/mL) for 2-72 hours. Cellular uptake is assessed by fluorescently labeled particles (flow cytometry, confocal microscopy). Cytotoxicity is measured by MTT or CCK-8. Folate-targeted micelles show enhanced uptake in folate receptor-positive cancer cells compared to non-targeted controls.
Animal Protocol
PEG-bis-amine-based nanoparticles or micelles (e.g., folate-conjugated 9-nitrocamptothecin-loaded micelles) are administered intravenously (tail vein injection) to tumor-bearing mice (typically 5-20 mg/kg polymer equivalent). Tumor volume is measured over time to assess antitumor efficacy. Biodistribution studies quantify drug accumulation in tumors versus healthy organs. Body weight and survival are monitored for safety assessment.
ADME/Pharmacokinetics
PEG-bis-amine has no intrinsic pharmacokinetics as it is a polymer vehicle. When conjugated to a drug, the conjugate's PK is determined by the molecular weight and surface chemistry. PEGylation (attachment of PEG) generally increases circulation half-life, reduces renal clearance, and decreases immunogenicity of the conjugated therapeutic agent. PK can be tailored by varying PEG MW and conjugation chemistry.
Toxicity/Toxicokinetics
PEG polymers, including PEG-bis-amine, are generally recognized as safe (GRAS) by the FDA for use in pharmaceuticals, medical devices, and cosmetics. At typical doses used in drug delivery formulations (10-100 mg/kg in animals), PEG-bis-amine is nontoxic. High doses may cause vacuolation in certain tissues but are generally reversible. PEG-related hypersensitivity is rare.
References

[1]. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

Additional Infomation
PEG-bis-amine (MW 8000) (CAS: 24991-53-5) is a research-grade polymer used for bioconjugation and drug delivery. It is available with various PEG chain lengths (MW 2000, 5000, 8000, 10000, 20000). It should be stored at 4degC, protected from light. It is not an approved drug itself, but PEG is widely used in FDA-approved PEGylated drugs and devices. The polymer is for research use only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
(C2H4O)NC4H12N2O
Molecular Weight
8000(Average)
Exact Mass
148.121
CAS #
24991-53-5
Appearance
White to off-white solid powder
Density
1.003g/cm3
Boiling Point
241ºC at 760mmHg
Flash Point
>110℃
LogP
0.337
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

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)
H2O : ~100 mg/mL
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.)
Calculator

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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?
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  • Enter 10 in the Concentration box and choose the correct unit (mM)
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  • 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
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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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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