Linker Information
General Information of This Linker
| Linker ID |
LIN0KDGHC
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
40i-5657 Linker
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C100H152F2N14O32
|
|||||
| Isosmiles |
CC(C)[C@@H](NC([C@H]1CCCN1C([C@H](NC(CCOCCOCCOCCNC(CCC(CCC(NC(CCOCCOCCOCCOCCNC(CCCC(C)=O)=O)=O)C(NCCOCCOCCOCCC(N/C(C(N2[C@@H](C(N[C@H](C(C)C)C(N[C@H](CCN([C@@H](C(C)(C)C)C3=CC(C4=C(F)C=CC(F)=C4)=CN3CC5=CC=CCC5)C(CO)=O)C(NC)=O)=O)=O)CCC2)=O)=C/C(O)=O)=O)=O)=O)=O)=O)CC(O)=O)=O)=O)C(O)=O
|
|||||
| InChI |
InChI=1S/C100H152F2N14O32/c1-65(2)89(96(134)110-75(92(130)103-9)28-37-116(86(125)64-117)91(100(6,7)8)80-58-69(72-59-70(101)22-25-73(72)102)63-113(80)62-68-17-11-10-12-18-68)111-94(132)78-19-14-35-114(78)97(135)76(60-87(126)127)108-84(123)30-39-141-45-51-146-55-49-144-43-34-106-93(131)74(107-83(122)29-38-139-46-52-147-56-57-148-54-48-142-41-32-104-81(120)21-13-16-67(5)118)26-23-71(119)24-27-82(121)105-33-42-143-47-53-145-50-44-140-40-31-85(124)109-77(61-88(128)129)98(136)115-36-15-20-79(115)95(133)112-90(66(3)4)99(137)138/h10-11,17,22,25,58-60,63,65-66,74-75,77-79,89-91,117H,12-16,18-21,23-24,26-57,61-62,64H2,1-9H3,(H,103,130)(H,104,120)(H,105,121)(H,106,131)(H,107,122)(H,108,123)(H,109,124)(H,110,134)(H,111,132)(H,112,133)(H,126,127)(H,128,129)(H,137,138)/b76-60+/t74?,75-,77-,78-,79-,89-,90-,91-/m1/s1
|
|||||
| InChIKey |
VIZOLHIMLVTSOK-MGZCLXGOSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
2100.378
|
Polar area
|
615.43
|
||
|
Complexity
|
.
|
xlogp Value
|
1.6896
|
|||
|
Heavy Count
|
148
|
Rot Bonds
|
77
|
|||
|
Hbond acc
|
30
|
Hbond Donor
|
14
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
WO2024105206A1 40p-Avelu 2 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
0.01- 1 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 38 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Renal cell carcinoma | 786-O cells (+NE) | CVCL_1051 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
0.01- 1 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 36 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Plasma cell myeloma, Multiple myeloma | NCI-H929 cells (+NE) | CVCL_1600 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
0.01- 1 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 36 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Breast inflammatory carcinoma | SUM149PT cells (+NE) | CVCL_3422 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
1.0- 9.9 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 41 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | HT29 cells (+NE) | CVCL_0320 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
10- 99 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 38 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Renal cell carcinoma | 786-O cells (-NE) | CVCL_1051 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
10- 99 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 21 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | HT29 cells (-NE) | CVCL_0320 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
10- 99 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 36 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Plasma cell myeloma, Multiple myeloma | NCI-H929 cells (-NE) | CVCL_1600 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
10- 99 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 36 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Breast inflammatory carcinoma | SUM149PT cells (-NE) | CVCL_3422 | ||