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| Targets |
Non-cleavable Linker
BCN-PEG3-Biotin contains a BCN group that enables fast, copper-free strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-functionalized molecules, making it ideal for bioorthogonal labeling under mild conditions. The biotin group provides strong, specific binding to streptavidin and avidin, enabling sensitive detection, purification, and immobilization applications. |
|---|---|
| ln Vitro |
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
In vitro, BCN-PEG3-Biotin is used for the labeling and detection of biomolecules. The BCN group reacts with azide-containing molecules via SPAAC, allowing for site-specific conjugation of biotin to target molecules. The biotin moiety then enables detection using streptavidin-based assays such as Western blotting, ELISA, or pull-down experiments. |
| ln Vivo |
In vivo activity data for BCN-PEG3-Biotin are primarily related to its use as an ADC linker or bioconjugation tool. The compound itself is not typically evaluated for therapeutic activity but rather for its ability to facilitate stable bioconjugation in biological systems.
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| Enzyme Assay |
For non-cellular in vitro assays, BCN-PEG3-Biotin is evaluated for its click chemistry reactivity. The compound is incubated with azide-functionalized molecules under physiological conditions, and the efficiency of the SPAAC reaction is monitored by HPLC, mass spectrometry, or fluorescence detection. The biotin-streptavidin binding affinity may also be assessed using surface plasmon resonance or ELISA.
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| Cell Assay |
For in vitro cellular assays, BCN-PEG3-Biotin is used to label cell surface proteins or internalized biomolecules that have been metabolically or enzymatically modified with azide groups. Cells are incubated with the compound, and biotinylation is detected using fluorescently labeled streptavidin and analyzed by flow cytometry or fluorescence microscopy.
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| Animal Protocol |
In vivo animal studies for BCN-PEG3-Biotin are typically conducted in the context of ADC efficacy or bioorthogonal labeling. The compound or its ADC conjugate is administered to animal models, and biodistribution, target engagement, and therapeutic efficacy are assessed using biotin-streptavidin detection systems.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BCN-PEG3-Biotin are primarily relevant in ADC development. The PEG3 spacer enhances solubility and flexibility while reducing steric hindrance. The non-cleavable nature of the linker provides stability in circulation.
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| Toxicity/Toxicokinetics |
BCN-PEG3-Biotin is generally considered to have low toxicity as a bioconjugation reagent. In ADC applications, the toxicity profile is determined by the overall ADC construct, including the antibody and payload. The compound itself is used in research settings for labeling and detection purposes.
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| References | |
| Additional Infomation |
BCN-PEG3-Biotin is a non-cleavable 3-unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It is a click chemistry reagent containing a BCN group that undergoes strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing azide groups. The compound has a molecular weight of 594.76 and a molecular formula of C₂₉H₄₆N₄O₇S.
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| Molecular Formula |
C29H46N4O7S
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|---|---|
| Molecular Weight |
594.76
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| Exact Mass |
594.308
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| CAS # |
1263166-92-2
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| PubChem CID |
57403826
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
847.5±65.0 °C at 760 mmHg
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| Flash Point |
466.4±34.3 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.574
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| LogP |
0.85
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
41
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| Complexity |
907
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1C[C@@H]2[C@@H](C2COC(=O)NCCOCCOCCOCCNC(=O)CCCC[C@H]3[C@@H]4[C@H](CS3)NC(=O)N4)CCC#C1
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| InChi Key |
LZIHJLCCQAFQSO-MSBMMZNKSA-N
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| InChi Code |
InChI=1S/C29H46N4O7S/c34-26(10-6-5-9-25-27-24(20-41-25)32-28(35)33-27)30-11-13-37-15-17-39-18-16-38-14-12-31-29(36)40-19-23-21-7-3-1-2-4-8-22(21)23/h21-25,27H,3-20H2,(H,30,34)(H,31,36)(H2,32,33,35)/t21-,22+,23?,24-,25-,27-/m0/s1
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| Chemical Name |
[(1S,8R)-9-bicyclo[6.1.0]non-4-ynyl]methyl N-[2-[2-[2-[2-[5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]ethoxy]ethoxy]ethoxy]ethyl]carbamate
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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) |
DMSO: 100 mg/mL (168.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6814 mL | 8.4068 mL | 16.8135 mL | |
| 5 mM | 0.3363 mL | 1.6814 mL | 3.3627 mL | |
| 10 mM | 0.1681 mL | 0.8407 mL | 1.6814 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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