1. Antibody-drug Conjugate/ADC Related PROTAC
  2. ADC Linker PROTAC Linkers
  3. 1-Boc-azetidine-3-yl-methanol

1-Boc-azetidine-3-yl-methanol is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-Boc-azetidine-3-yl-methanol is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]

For research use only. We do not sell to patients.

1-Boc-azetidine-3-yl-methanol Chemical Structure

1-Boc-azetidine-3-yl-methanol Chemical Structure

CAS No. : 142253-56-3

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

1-Boc-azetidine-3-yl-methanol is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-Boc-azetidine-3-yl-methanol is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]

IC50 & Target

Non-cleavable Linker

 

In Vitro

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

187.24

Formula

C9H17NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC(C)(C)C)N1CC(CO)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (534.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.3407 mL 26.7037 mL 53.4074 mL
5 mM 1.0681 mL 5.3407 mL 10.6815 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (13.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.3407 mL 26.7037 mL 53.4074 mL 133.5185 mL
5 mM 1.0681 mL 5.3407 mL 10.6815 mL 26.7037 mL
10 mM 0.5341 mL 2.6704 mL 5.3407 mL 13.3518 mL
15 mM 0.3560 mL 1.7802 mL 3.5605 mL 8.9012 mL
20 mM 0.2670 mL 1.3352 mL 2.6704 mL 6.6759 mL
25 mM 0.2136 mL 1.0681 mL 2.1363 mL 5.3407 mL
30 mM 0.1780 mL 0.8901 mL 1.7802 mL 4.4506 mL
40 mM 0.1335 mL 0.6676 mL 1.3352 mL 3.3380 mL
50 mM 0.1068 mL 0.5341 mL 1.0681 mL 2.6704 mL
60 mM 0.0890 mL 0.4451 mL 0.8901 mL 2.2253 mL
80 mM 0.0668 mL 0.3338 mL 0.6676 mL 1.6690 mL
100 mM 0.0534 mL 0.2670 mL 0.5341 mL 1.3352 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
1-Boc-azetidine-3-yl-methanol
Cat. No.:
HY-40152
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