General Information of This Linker
Linker ID
LIN0ZLYAJ
Linker Name
DIBAC-PEG4 linker
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Formula
C41H57N7O10
Isosmiles
CC([C@H](NC(CCOCCOCCOCCOCCNC(CCC(N1C2=C(C#CC(C=CC=C3)=C3C1)C=CC=C2)=O)=O)=O)C(N[C@@H](CCCNC(N)=O)C(N)=O)=O)C
InChI
InChI=1S/C41H57N7O10/c1-29(2)38(40(53)46-33(39(42)52)11-7-18-45-41(43)54)47-36(50)17-20-55-22-24-57-26-27-58-25-23-56-21-19-44-35(49)15-16-37(51)48-28-32-10-4-3-8-30(32)13-14-31-9-5-6-12-34(31)48/h3-6,8-10,12,29,33,38H,7,11,15-28H2,1-2H3,(H2,42,52)(H,44,49)(H,46,53)(H,47,50)(H3,43,45,54)/t33-,38-/m0/s1
InChIKey
NRFUVIQMSIYOPS-BAOFOTJISA-N
Pharmaceutical Properties
Molecule Weight
807.946
Polar area
242.74
Complexity
1660.535962
xlogp Value
0.8453
Heavy Count
58
Rot Bonds
27
Hbond acc
10
Hbond Donor
6
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
TRSQ-ZP3A- LP6-Vb [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.046 nM
Positive HER2 expression (HER2+++/++)
Method Description
The anti-proliferation test was carried out with SK-BR-3 human breast cancer cell line. Cells were grown in McCoy's 5a medium supplemented with 43% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
TRSQ-ZP3A-LP22 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.376 nM
Positive HER2 expression (HER2+++/++)
Method Description
The anti-proliferation test was carried out with SK-BR-3 human breast cancer cell line. Cells were grown in McCoy's 5a medium supplemented with 27% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
TRSQ-ZP3A-LP24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.733 nM
Positive HER2 expression (HER2+++/++)
Method Description
The anti-proliferation test was carried out with SK-BR-3 human breast cancer cell line. Cells were grown in McCoy's 5a medium supplemented with 30% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
CTRL-ZP3A-LP24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
321.547 nM
Positive HER2 expression (HER2+++/++)
Method Description
The anti-proliferation test was carried out with SK-BR-3 human breast cancer cell line. Cells were grown in McCoy's 5a medium supplemented with 31% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
CTRL-ZP3A-LP22 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
461.721 nM
Positive HER2 expression (HER2+++/++)
Method Description
The anti-proliferation test was carried out with SK-BR-3 human breast cancer cell line. Cells were grown in McCoy's 5a medium supplemented with 28% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
References
Ref 1 Tubulysins and protein-tubulysin conjugates