Linker Information
General Information of This Linker
| Linker ID |
LIN0IGGBB
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| Linker Name |
Ala-Gln linker
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C10H16BrN3O5
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| Isosmiles |
OC([C@H](CCC(N)=O)NC([C@H](C)NC(CBr)=O)=O)=O
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| InChI |
InChI=1S/C10H16BrN3O5/c1-5(13-8(16)4-11)9(17)14-6(10(18)19)2-3-7(12)15/h5-6H,2-4H2,1H3,(H2,12,15)(H,13,16)(H,14,17)(H,18,19)/t5-,6-/m0/s1
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| InChIKey |
UFMNDOMHEPJLTJ-WDSKDSINSA-N
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| Pharmaceutical Properties |
Molecule Weight
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338.158
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Polar area
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138.59
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Complexity
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343.0498112
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xlogp Value
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-1.2791
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Heavy Count
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19
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Rot Bonds
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8
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Hbond acc
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4
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Hbond Donor
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4
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
38283215 ADC 3 [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) |
0.95 ug/mL
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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.
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| 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) | > 15 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.
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| In Vitro Model | Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia | K562 cells (wt) | CVCL_0004 | ||
References