Linker Information
General Information of This Linker
| Linker ID |
LIN0DZEKU
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| Linker Name |
Conjugate No.112 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 |
C42H72N10O24
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| Isosmiles |
O=C(NCC(NC(CO)C(NC(C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)=O)CCC(NC[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO)O)=O)=O)CNC(CNC(CNC(CCOCCOCCNC(CCN1C(C=CC1=O)=O)=O)=O)=O)=O
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| InChI |
InChI=1S/C42H72N10O24/c53-19-23(42(74)51-22(41(73)49-14-25(57)38(70)40(72)27(59)21-55)1-2-28(60)44-13-24(56)37(69)39(71)26(58)20-54)50-34(66)18-48-33(65)17-47-32(64)16-46-31(63)15-45-30(62)6-9-75-11-12-76-10-7-43-29(61)5-8-52-35(67)3-4-36(52)68/h3-4,22-28,37-40,44,53-60,69-72H,1-2,5-21H2,(H,43,61)(H,45,62)(H,46,63)(H,47,64)(H,48,65)(H,49,73)(H,50,66)(H,51,74)/t22?,23?,24-,25-,26-,27+,28?,37+,38+,39+,40+/m0/s1
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| InChIKey |
ITEUTIQBILDJAW-JENUKTEQSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1101.084
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Polar area
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543.43
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Complexity
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1780.756826
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xlogp Value
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-14.0561
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Heavy Count
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76
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Rot Bonds
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41
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Hbond acc
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25
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Hbond Donor
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21
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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.112 [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) |
0.02 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) |
0.13 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) |
0.68 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 | ||