Linker Information
General Information of This Linker
| Linker ID |
LIN0QRNFV
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| Linker Name |
Conjugate No.94 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 |
C47H76N12O26
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| Isosmiles |
C[C@H](NC([C@@H](NC(CC[C@H](NC(CN1C(C=CC1=O)=O)=O)C(NCC(NCC(NCC(NCC(NCCOCCC(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)=O)=O)=O)=O)=O)C)=O)C(O)=O
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| InChI |
InChI=1S/C47H76N12O26/c1-22(44(80)56-23(2)47(83)84)55-31(67)6-4-25(58-37(73)19-59-38(74)7-8-39(59)75)46(82)54-18-36(72)52-17-35(71)51-16-34(70)50-15-33(69)48-10-12-85-11-9-32(68)57-24(45(81)53-14-27(63)41(77)43(79)29(65)21-61)3-5-30(66)49-13-26(62)40(76)42(78)28(64)20-60/h7-8,22-29,40-43,60-65,76-79H,3-6,9-21H2,1-2H3,(H,48,69)(H,49,66)(H,50,70)(H,51,71)(H,52,72)(H,53,81)(H,54,82)(H,55,67)(H,56,80)(H,57,68)(H,58,73)(H,83,84)/t22-,23-,24?,25-,26-,27-,28+,29+,40+,41+,42+,43+/m0/s1
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| InChIKey |
LYWGKFZFJJNHIT-PYOFICHRSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1225.183
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Polar area
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606.31
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Complexity
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2212.510915
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xlogp Value
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-14.3727
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Heavy Count
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85
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Rot Bonds
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42
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Hbond acc
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25
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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.94 [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) |
0.07 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) |
1.35 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 | ||
WO2019126691A1 Conjugate No.94A [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) |
0.08 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
OVCAR3 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 | High grade ovarian serous adenocarcinoma | OVCAR3 cells | CVCL_0465 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
20.5 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 | ||
WO2019126691A1 Conjugate No.94B [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) |
3.19 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 | ||