2. Antibody-drug Conjugate/ADC Related
  3. ADC Linker
  4. DBCO-amine

DBCO-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-amine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

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DBCO-amine Chemical Structure

DBCO-amine Chemical Structure

CAS No. : 1255942-06-3

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Based on 1 publication(s) in Google Scholar

Other Forms of DBCO-amine:

DBCO-amine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DBCO-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. DBCO-amine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

IC50 & Target[1]

Cleavable Linker

 

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
32.06 μM
Compound: 4
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
[PMID: 27769619]
MCF7 IC50
28 μM
Compound: 4
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
[PMID: 27769619]
MRC5 IC50
60.4 μM
Compound: 4
Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay
Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay
[PMID: 27769619]
In Vitro

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.

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

DBCO-amine Related Antibodies
Molecular Weight

276.33

Formula

C18H16N2O
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(N1C2=CC=CC=C2C#CC3=CC=CC=C3C1)CCN
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (361.89 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 3.6189 mL 18.0943 mL 36.1886 mL
5 mM 0.7238 mL 3.6189 mL 7.2377 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 (protect from light). 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 (9.05 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.05 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.11%

SDS (393 KB)

COA (251 KB) HNMR (256 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 3.6189 mL 18.0943 mL 36.1886 mL 90.4715 mL
5 mM 0.7238 mL 3.6189 mL 7.2377 mL 18.0943 mL
10 mM 0.3619 mL 1.8094 mL 3.6189 mL 9.0472 mL
15 mM 0.2413 mL 1.2063 mL 2.4126 mL 6.0314 mL
20 mM 0.1809 mL 0.9047 mL 1.8094 mL 4.5236 mL
25 mM 0.1448 mL 0.7238 mL 1.4475 mL 3.6189 mL
30 mM 0.1206 mL 0.6031 mL 1.2063 mL 3.0157 mL
40 mM 0.0905 mL 0.4524 mL 0.9047 mL 2.2618 mL
50 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8094 mL
60 mM 0.0603 mL 0.3016 mL 0.6031 mL 1.5079 mL
80 mM 0.0452 mL 0.2262 mL 0.4524 mL 1.1309 mL
100 mM 0.0362 mL 0.1809 mL 0.3619 mL 0.9047 mL
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DBCO-amine Related Classifications

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.

Keywords:

DBCO-amine1255942-06-3ADC LinkerAntibody-drug conjugates linkernon-cleavableADCantibody-drugconjugatesInhibitorinhibitorinhibit

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