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| 1mg |
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| 5mg |
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| Targets |
The compound is a linker and fluorescent dye, not a drug with a specific biological target. It is classified as a PROTAC linker. The carboxylic acid group allows it to react with primary amine groups to form stable amide bonds. In the context of PROTACs, it acts as a linker that brings together two ligands, one targeting the protein of interest and the other recruiting an E3 ubiquitin ligase.
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| ln Vitro |
Two distinct ligands, one for the E3 ubiquitin ligase and the other for the target protein, are present in PROTAC and are joined by a linker. PROTAC selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system [1].
The compound does not possess direct biological activity as it is a linker. Its in vitro utility lies in its ability to form stable conjugates with biomolecules via amide bond formation. The PEG4 spacer increases solubility in aqueous media. It is used to label proteins and peptides, helping to study protein-protein interactions, cellular localization, and protein dynamics. |
| ln Vivo |
The compound is a chemical reagent and does not have direct in vivo biological activity. Its utility in vivo is as a component of PROTACs or other bioconjugates, where it links pharmacologically active moieties and provides a fluorescent label. PEGylation is known to improve the pharmacokinetics of drugs by increasing solubility and prolonging circulation time.
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| Enzyme Assay |
As a chemical linker, the compound is not used in biological enzyme assays. Its utility lies in chemical conjugation reactions. The carboxylic acid group can be activated with EDC or HATU to form amide bonds with primary amines. The reaction is typically carried out in suitable buffers at room temperature. Conjugation efficiency is monitored by HPLC or LC-MS.
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| Cell Assay |
For in vitro cell-based assays using PROTACs synthesized with this linker, target cells are treated with the PROTAC at various concentrations for 24-72 hours. Target protein degradation is assessed by Western blot analysis. Cell viability is measured using MTT or similar assays. The TAMRA fluorophore allows for visualization by fluorescence microscopy.
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| ADME/Pharmacokinetics |
TAMRA-PEG4-acid (CAS 1909223-02-4) has a molecular formula of C36H43N3O10 and a molecular weight of 677.8. It is soluble in DMSO, DMF, and DCM. It should be stored at -20°C. The compound is a solid powder. Detailed pharmacokinetic parameters are not applicable as the compound is a linker.
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| Toxicity/Toxicokinetics |
As a chemical linker and fluorescent dye, the compound is not a pharmacologically active compound and does not have direct toxicity. Toxicity would be associated with the final therapeutic agents synthesized using this linker. The PEG component is generally considered biocompatible and non-toxic. No specific toxicity data are provided.
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| References | |
| Additional Infomation |
TAMRA-PEG4-acid is a TAMRA red-fluorescent dye derivative used for labeling and tracking molecules. It is used in the development of PROTACs, which are designed to selectively degrade target proteins, with potential therapeutic applications in treating diseases such as cancer and neurodegenerative disorders. It is also used in the production of diagnostic kits and imaging agents.
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| Exact Mass |
677.294
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| CAS # |
1909223-02-4
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| PubChem CID |
129627640
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| Appearance |
Brown to reddish brown liquid
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
49
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| Complexity |
1220
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AZESQZROUFRXLP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C36H43N3O10/c1-38(2)25-6-9-28-31(22-25)49-32-23-26(39(3)4)7-10-29(32)34(28)27-8-5-24(21-30(27)36(43)44)35(42)37-12-14-46-16-18-48-20-19-47-17-15-45-13-11-33(40)41/h5-10,21-23H,11-20H2,1-4H3,(H2-,37,40,41,42,43,44)
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| Chemical Name |
5-[2-[2-[2-[2-(2-carboxyethoxy)ethoxy]ethoxy]ethoxy]ethylcarbamoyl]-2-[3-(dimethylamino)-6-dimethylazaniumylidenexanthen-9-yl]benzoate
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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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