Linker Information
General Information of This Linker
| Linker ID |
LIN0HRPQL
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| Linker Name |
Ala-Arg 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 |
C11H20BrN5O4
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| Isosmiles |
OC([C@H](CCC/N=C(N)\N)NC([C@H](C)NC(CBr)=O)=O)=O
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| InChI |
InChI=1S/C11H20BrN5O4/c1-6(16-8(18)5-12)9(19)17-7(10(20)21)3-2-4-15-11(13)14/h6-7H,2-5H2,1H3,(H,16,18)(H,17,19)(H,20,21)(H4,13,14,15)/t6-,7-/m0/s1
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| InChIKey |
FUKYPIURTXAEDX-BQBZGAKWSA-N
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| Pharmaceutical Properties |
Molecule Weight
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366.216
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Polar area
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159.9
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Complexity
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376.842491
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xlogp Value
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-1.491
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Heavy Count
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21
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Rot Bonds
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9
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Hbond acc
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4
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Hbond Donor
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5
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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 2 [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) |
0.74 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) | > 50 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