General Information of This Linker
Linker ID
LIN0SBGBK
Linker Name
ADC-P1 BGB-C-269 Linker
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C37H51N7O15
Isosmiles
O=C(NCC(NCC(N[C@@H](CC1=CC=CC=C1)C(NCC(O)=O)=O)=O)=O)[C@@H](NC(CCCCCN2C(C=CC2=O)=O)=O)CCC(NC[C@H](O3)[C@H](O)[C@@H](O)[C@H](O)[C@H]3CO)=O
InChI
InChI=1S/C37H51N7O15/c45-20-25-34(55)35(56)33(54)24(59-25)16-38-26(46)11-10-22(42-27(47)9-5-2-6-14-44-30(50)12-13-31(44)51)36(57)40-17-28(48)39-18-29(49)43-23(37(58)41-19-32(52)53)15-21-7-3-1-4-8-21/h1,3-4,7-8,12-13,22-25,33-35,45,54-56H,2,5-6,9-11,14-20H2,(H,38,46)(H,39,48)(H,40,57)(H,41,58)(H,42,47)(H,43,49)(H,52,53)/t22-,23-,24-,25+,33-,34+,35+/m0/s1
InChIKey
WSSARPLLWUREJB-HENUYNGUSA-N
Pharmaceutical Properties
Molecule Weight
833.849
Polar area
339.43
Complexity
1598.298893
xlogp Value
-5.1439
Heavy Count
59
Rot Bonds
24
Hbond acc
14
Hbond Donor
11
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
BGA0084 [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)
0.19 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)
0.38 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)
0.85 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)
25 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