Linker Information
General Information of This Linker
| Linker ID |
LIN0UJSYD
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| Linker Name |
Conjugate No.119 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 |
C22H31N7O11
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| Isosmiles |
O=C(NCC(NCC(NCC(NCC(NCCOC)=O)=O)=O)=O)[C@@H](NC(CN1C(C=CC1=O)=O)=O)CCC(O)=O
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| InChI |
InChI=1S/C22H31N7O11/c1-40-7-6-23-14(30)8-24-15(31)9-25-16(32)10-26-17(33)11-27-22(39)13(2-5-21(37)38)28-18(34)12-29-19(35)3-4-20(29)36/h3-4,13H,2,5-12H2,1H3,(H,23,30)(H,24,31)(H,25,32)(H,26,33)(H,27,39)(H,28,34)(H,37,38)/t13-/m0/s1
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| InChIKey |
GXPMYVPMRDQNLZ-ZDUSSCGKSA-N
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| Pharmaceutical Properties |
Molecule Weight
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569.528
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Polar area
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258.51
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Complexity
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969.0557005
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xlogp Value
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-5.5116
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Heavy Count
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40
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Rot Bonds
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18
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Hbond acc
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10
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Hbond Donor
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7
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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
WO2019126691A1 Conjugate No.119 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.06 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Lung adenocarcinoma | Calu3 cells | CVCL_0609 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.49 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Breast ductal carcinoma | JIMT1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
6.36 nM
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Low HER2 expression (HER2+) | ||
| Method Description |
MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||