Linker Information
General Information of This Linker
| Linker ID |
LIN0MTENM
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| Linker Name |
Conjugate No.115 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 |
C61H109N11O33
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| Isosmiles |
O=C(N1CCC(NCCOCCOCCC(NCC(NCC(NCC(NCC(NC(CO)C(NCCOCCOCCOCCOCCOCCOCCOCCOCCC(NC(CCC(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)O)C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)=O)=O)=O)=O)=O)=O)=O)=O)=O)C=CC1=O
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| InChI |
InChI=1S/C61H109N11O33/c73-37-41(71-53(87)36-68-52(86)35-67-51(85)34-66-50(84)33-65-48(82)6-11-96-15-17-98-13-8-62-47(81)5-10-72-54(88)3-4-55(72)89)61(95)63-9-14-99-18-20-101-22-24-103-26-28-105-30-29-104-27-25-102-23-21-100-19-16-97-12-7-49(83)70-40(60(94)69-32-43(77)57(91)59(93)45(79)39-75)1-2-46(80)64-31-42(76)56(90)58(92)44(78)38-74/h3-4,40-46,56-59,64,73-80,90-93H,1-2,5-39H2,(H,62,81)(H,63,95)(H,65,82)(H,66,84)(H,67,85)(H,68,86)(H,69,94)(H,70,83)(H,71,87)/t40?,41?,42-,43-,44+,45+,46?,56+,57+,58+,59+/m0/s1
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| InChIKey |
AEDITVCNMHGLSZ-RFQQCKGXSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1524.587
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Polar area
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646.37
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Complexity
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2347.277058
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xlogp Value
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-14.417
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Heavy Count
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105
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Rot Bonds
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68
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Hbond acc
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34
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Hbond Donor
|
22
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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.115 [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) |
0.03 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) |
0.18 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) |
0.89 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 | ||