Linker Information
General Information of This Linker
| Linker ID |
LIN0ZFCJA
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
Val-Gly linker
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C9H15BrN2O4
|
|||||
| Isosmiles |
OC(C([H])NC([C@H](C(C)C)NC(CBr)=O)=O)=O
|
|||||
| InChI |
InChI=1S/C9H15BrN2O4/c1-5(2)8(12-6(13)3-10)9(16)11-4-7(14)15/h5,8H,3-4H2,1-2H3,(H,11,16)(H,12,13)(H,14,15)/t8-/m0/s1
|
|||||
| InChIKey |
QSLMHWYITAWUOK-QMMMGPOBSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
295.133
|
Polar area
|
95.5
|
||
|
Complexity
|
255.2118756
|
xlogp Value
|
-0.2771
|
|||
|
Heavy Count
|
16
|
Rot Bonds
|
6
|
|||
|
Hbond acc
|
3
|
Hbond Donor
|
3
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
38283215 ADC 26 [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) |
0.55 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