Linker Information
General Information of This Linker
| Linker ID |
LIN0VEXOD
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| Linker Name |
AU2023281032A1 ADC-1 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 |
C39H63N9O15
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| Isosmiles |
OCC(OC1OC(NC1C2CO)C)C2OC[C@@H](CC(CC(NCC(NCC(NCC(N[C@@H](C(C)C)C(N[C@H](C(NC3=CC=C(C=C3)CO)=O)CCCNC(N)=O)=O)=O)=O)=O)=O)O)O
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| InChI |
InChI=1S/C39H63N9O15/c1-20(2)33(37(59)47-27(5-4-10-41-39(40)60)36(58)46-23-8-6-22(16-49)7-9-23)48-32(57)15-44-31(56)14-43-30(55)13-42-29(54)12-24(52)11-25(53)19-61-35-26(17-50)34-38(62-21(3)45-34)63-28(35)18-51/h6-9,20-21,24-28,33-35,38,45,49-53H,4-5,10-19H2,1-3H3,(H,42,54)(H,43,55)(H,44,56)(H,46,58)(H,47,59)(H,48,57)(H3,40,41,60)/t21?,24?,25-,26?,27+,28?,33+,34?,35?,38?/m1/s1
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| InChIKey |
FGUWEKRWHPMDBT-GSKCLWTDSA-N
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| Pharmaceutical Properties |
Molecule Weight
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897.981
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Polar area
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370.59
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Complexity
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1590.109774
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xlogp Value
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-4.9126
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Heavy Count
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63
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Rot Bonds
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26
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Hbond acc
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16
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Hbond Donor
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14
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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
AU2023281032A1 ADC-5 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
25.61%
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| Method Description |
Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in HepG2
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| In Vivo Model | HepG2 CDX Mouse Model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
72.22%
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| Method Description |
Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in FaDu
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| In Vivo Model | FaDu CDX Mouse Model | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
98.21%
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| Method Description |
Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in BxPC-3
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| In Vivo Model | BxPC-3 CDX Mouse Model | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
98.21%
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| Method Description |
Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in BxPC-3
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| In Vivo Model | BxPC-3 CDX Mouse Model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.1017 nM
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| Method Description |
Proliferation Inhibition Action of Different Drugs on Tumor Cells (IC50, nM) in BxPC-3
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| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
AU2023281032A1 ADC-1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
115.07%
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| Method Description |
Inhibition Effect of ADC-1,3mg/kg on NCI-N87 CDX Mouse Model
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| In Vivo Model | NCI-N87 CDX Mouse Model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.04636 nM
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| Method Description |
Proliferation Inhibition Effect of Different Drugs on Tumor Cells (IC50, nM)in BT-474,
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.08706 nM
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| Method Description |
Proliferation Inhibition Effect of Different Drugs on Tumor Cells (IC50, nM)in NCI-N87
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References