General Information of This Linker
Linker ID
LIN0BSULK
Linker Name
Dimaleimide linker 3
Linker Type
Uncleavable linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C12H12N2O4
Isosmiles
O=C1C=CC(N1CCCCN2C(C=CC2=O)=O)=O
PubChem CID
239576
InChI
InChI=1S/C12H12N2O4/c15-9-3-4-10(16)13(9)7-1-2-8-14-11(17)5-6-12(14)18/h3-6H,1-2,7-8H2
InChIKey
WXXSHAKLDCERGU-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
248.238
Polar area
74.76
Complexity
376.4299824
xlogp Value
-0.3834
Heavy Count
18
Rot Bonds
5
Hbond acc
4
Hbond Donor
0
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
38850783 ADC 3 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Ninety Percent Inhibitory Concentration (IC90)
0.11- 0.28 ng/mL
Negative HER2 expression (HER2-)
Method Description
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).

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In Vitro Model Breast ductal carcinoma HCC1937 cells CVCL_0290
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Ninety Percent Inhibitory Concentration (IC90)
0.27- 0.38 ng/mL
High HER2 expression (HER2 +++)
Method Description
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.18 ng/mL
Negative HER2 expression (HER2-)
Method Description
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).

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In Vitro Model Breast ductal carcinoma HCC1937 cells CVCL_0290
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.32 ng/mL
High HER2 expression (HER2 +++)
Method Description
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
References
Ref 1 Synthesis and evaluation of antibody-drug conjugates with high drug-to-antibody ratio using dimaleimide-DM1 as a linker- payload