Linker Information
General Information of This Linker
| Linker ID |
LIN0WWPAP
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
Val-Gln linker
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C12H20BrN3O5
|
|||||
| Isosmiles |
OC([C@H](CCC(N)=O)NC([C@H](C(C)C)NC(CBr)=O)=O)=O
|
|||||
| InChI |
InChI=1S/C12H20BrN3O5/c1-6(2)10(16-9(18)5-13)11(19)15-7(12(20)21)3-4-8(14)17/h6-7,10H,3-5H2,1-2H3,(H2,14,17)(H,15,19)(H,16,18)(H,20,21)/t7-,10-/m0/s1
|
|||||
| InChIKey |
SEKWBLSPHROZNV-XVKPBYJWSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
366.212
|
Polar area
|
138.59
|
||
|
Complexity
|
380.842491
|
xlogp Value
|
-0.643
|
|||
|
Heavy Count
|
21
|
Rot Bonds
|
9
|
|||
|
Hbond acc
|
4
|
Hbond Donor
|
4
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
38283215 ADC 24 [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) |
1.26 ug/mL
|
High TNF expression (TNF +++) | ||
| Method Description |
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.
Click to Show/Hide
|
||||
| In Vitro Model | Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia | K562 cells (TNF) | CVCL_0004 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 19 ug/mL | Negative TNF expression (TNF-) | ||
| Method Description |
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.
Click to Show/Hide
|
||||
| In Vitro Model | Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia | K562 cells (wt) | CVCL_0004 | ||
References