General Information of This Linker
Linker ID
LIN0OKZMX
Linker Name
DIBAC-PEG4-vcPAB
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C57H83N11O16
Isosmiles
CC([C@H](NC(CCOCCOCCOCCOCCNC(CCC(N1CC2=C(C(NNN3CCOCCOCCOCCN)=C3C4=C1C=CC=C4)C=CC=C2)=O)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC5=CC=C(C=C5)COC(O)=O)=O)=O)C
InChI
InChI=1S/C57H83N11O16/c1-40(2)51(55(73)63-46(11-7-21-61-56(59)74)54(72)62-43-15-13-41(14-16-43)39-84-57(75)76)64-49(70)19-24-77-28-32-81-36-37-83-34-30-79-26-22-60-48(69)17-18-50(71)67-38-42-8-3-4-9-44(42)52-53(45-10-5-6-12-47(45)67)68(66-65-52)23-27-80-31-35-82-33-29-78-25-20-58/h3-6,8-10,12-16,40,46,51,65-66H,7,11,17-39,58H2,1-2H3,(H,60,69)(H,62,72)(H,63,73)(H,64,70)(H,75,76)(H3,59,61,74)/t46-,51-/m0/s1
InChIKey
AQTXBWONYHXSFN-YWHGXOANSA-N
Pharmaceutical Properties
Molecule Weight
1178.352
Polar area
356.29
Complexity
2473.210765
xlogp Value
1.9526
Heavy Count
84
Rot Bonds
41
Hbond acc
19
Hbond Donor
10
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
TRSQ-ZP3A- LP15-Vlh [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)
0.044 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 46% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
TRSQ-ZP3A- LP4-Ve [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)
0.064 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 32% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
TRSQ-ZP3A-LP13 [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)
0.083 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 19% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
TRSQ-ZP3A-LP25 [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)
1.329 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 29% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
TRSQ-ZP3A-LP20 [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)
1.366 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 25% FBS,penicillin/streptomycin and L-glutamine.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
CTRL-ZP3A-LP4-Ve [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)
23.401 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 33% 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