General Information of This Linker
Linker ID
LIN0EDMZI
Linker Name
BGA7413 Linker
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C23H28N4O11S
Isosmiles
CC([C@H](NC(C1=CC=C(C2=NSC=N2)C=C1)=O)C(N[C@@H](CO[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](C(O)=O)O3)C(O)=O)=O)C
InChI
InChI=1S/C23H28N4O11S/c1-9(2)13(26-19(31)11-5-3-10(4-6-11)18-24-8-39-27-18)20(32)25-12(21(33)34)7-37-23-16(30)14(28)15(29)17(38-23)22(35)36/h3-6,8-9,12-17,23,28-30H,7H2,1-2H3,(H,25,32)(H,26,31)(H,33,34)(H,35,36)/t12-,13-,14-,15-,16+,17-,23+/m0/s1
InChIKey
UVQNJEUCNMSWKM-DEVNHDCCSA-N
Pharmaceutical Properties
Molecule Weight
568.561
Polar area
237.73
Complexity
1105.297973
xlogp Value
-1.5623
Heavy Count
39
Rot Bonds
11
Hbond acc
12
Hbond Donor
7
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
BGA7413 [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 Half Maximal Effective Concentration (EC50)
0.16 nM
Positive CEA expression (CEA+++/++)
Method Description
NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Lung adenocarcinoma NCI-H2122 cells CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.46 nM
Positive CEA expression (CEA+++/++)
Method Description
MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.88 nM
Positive CEA expression (CEA+++/++)
Method Description
Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Colon adenocarcinoma Ls147T cells CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
28 nM
Negative CEA expression (CEA-)
Method Description
MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Anti-CEA antibody drug conjugates and methods of use