Linker Information
General Information of This Linker
| Linker ID |
LIN0WHYYZ
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
BGA2490 Linker
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C29H39N7O10S
|
|||||
| Isosmiles |
CC([C@H](NC([C@@H](NC(C1=CC=C(C=C1)C2=NSC=N2)=O)CCC(NC[C@@H](O3)C(O)[C@@H](O)[C@@H]3CC(N)=O)=O)=O)C(N[C@@H](C)C(O)=O)=O)C
|
|||||
| InChI |
InChI=1S/C29H39N7O10S/c1-13(2)22(28(43)33-14(3)29(44)45)35-27(42)17(34-26(41)16-6-4-15(5-7-16)25-32-12-47-36-25)8-9-21(38)31-11-19-24(40)23(39)18(46-19)10-20(30)37/h4-7,12-14,17-19,22-24,39-40H,8-11H2,1-3H3,(H2,30,37)(H,31,38)(H,33,43)(H,34,41)(H,35,42)(H,44,45)/t14-,17-,18-,19+,22-,23-,24?/m0/s1
|
|||||
| InChIKey |
LPCOTXGDTVAFOQ-PTLUUGEMSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
677.737
|
Polar area
|
272.26
|
||
|
Complexity
|
1355.494829
|
xlogp Value
|
-1.7054
|
|||
|
Heavy Count
|
47
|
Rot Bonds
|
16
|
|||
|
Hbond acc
|
12
|
Hbond Donor
|
8
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
BGA2490 [Investigative]
Revealed Based on the Cell Line Data
| 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) |
0.44 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) |
0.76 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) |
21 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 | ||