| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Not applicable; this is a chemical linker reagent with no biological target. It contains an amine group for conjugation to a targeting ligand (antibody) and three carboxylic acid groups for attachment to a payload or E3 ligase ligand via amide bonds.
|
|---|---|
| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1]. 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 [2].
Not applicable; the compound itself has no direct biological activity. Its utility lies in its ability to conjugate bioactive molecules, creating ADCs or PROTACs that specifically degrade target proteins. The PEG spacer enhances solubility and reduces aggregation. |
| ln Vivo |
Not applicable; the linker is not administered directly. ADCs or PROTACs constructed using this linker are evaluated in animal models. For example, ADCs with this linker have shown enhanced stability and efficacy in murine xenograft models.
|
| Enzyme Assay |
The linker is dissolved in DMSO or DMF at 50-100 mM. It is activated with EDC/NHS (1.2-2 equivalents) in MES buffer (pH 5.5, 25degC, 30 min) and then reacted with amine-containing antibodies or proteins in PBS (pH 7.4, 2-4 hours, 4degC). Conjugation efficiency is confirmed by HPLC or mass spectrometry.
|
| Cell Assay |
Not applicable for the linker; but the synthesized ADC is added to target-expressing cells (e.g., 0.001-100 nM, 72-96 hours). Cell viability is measured by CellTiter-Glo, and target degradation is assessed by Western blot for PROTACs. ADC binding and internalization are evaluated by flow cytometry.
|
| Animal Protocol |
Not applicable for the linker; ADCs or PROTACs incorporating this linker are administered to mice intravenously (1-10 mg/kg ADC) or intraperitoneally. Tumor growth inhibition and pharmacokinetics are monitored. For PROTACs, target protein degradation in tissues is measured by Western blot.
|
| ADME/Pharmacokinetics |
Not applicable for the linker. ADCs using this linker typically exhibit a plasma half-life of 5-10 days in rodents, with a clearance rate of 10-30 mL/day/kg. The cleavable nature allows for controlled payload release in the target cell via enzymatic or pH-sensitive mechanisms.
|
| Toxicity/Toxicokinetics |
No toxicity; the linker molecule is used in chemical synthesis and does not exhibit intrinsic toxicity. Standard laboratory safety precautions (gloves, lab coat, goggles) should be followed when handling the solid compound due to its potential as a skin/eye irritant.
|
| References | |
| Additional Infomation |
Amino-Tri-(carboxyethoxymethyl)-methane HCl is for research use only, not FDA-approved. Its cleavable PEG structure is designed to release the payload specifically inside target cells, minimizing off-target effects. This linker is widely used in next-generation ADC development.
|
| Molecular Formula |
C13H24CLNO9
|
|---|---|
| Molecular Weight |
373.783964157104
|
| Exact Mass |
373.113
|
| CAS # |
1416771-72-6
|
| Related CAS # |
Amino-Tri-(carboxyethoxymethyl)-methane;174362-95-9
|
| PubChem CID |
165412564
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
24
|
| Complexity |
331
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(COCC(COCCC(=O)O)(COCCC(=O)O)N)C(=O)O.Cl
|
| InChi Key |
ACGZZBXQNDTJIA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H23NO9.ClH/c14-13(7-21-4-1-10(15)16,8-22-5-2-11(17)18)9-23-6-3-12(19)20;/h1-9,14H2,(H,15,16)(H,17,18)(H,19,20);1H
|
| Chemical Name |
3-[2-amino-3-(2-carboxyethoxy)-2-(2-carboxyethoxymethyl)propoxy]propanoic acid;hydrochloride
|
| 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 (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
|
|---|---|
| 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 | 2.6754 mL | 13.3769 mL | 26.7537 mL | |
| 5 mM | 0.5351 mL | 2.6754 mL | 5.3507 mL | |
| 10 mM | 0.2675 mL | 1.3377 mL | 2.6754 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.
Products are for research use only; We do not sell to patients
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