Linker Information
General Information of This Linker
| Linker ID |
LIN0VBBUR
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| Linker Name |
CN112341521B+Linker3
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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 |
C48H74N10O18S
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| Isosmiles |
CS(C1=NC(CN2CCCC(N=N3)=CN3CCOCCOCCOCCOCCOCCOCCOCCOCCNC(COCC(N[C@H](C(NC4=CC=C(COC(O)=O)C=C4)=O)CCCCN)=O)=O)=C(C2=O)C=N1)(=O)=O
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| InChI |
InChI=1S/C48H74N10O18S/c1-77(65,66)47-51-31-40-42(54-47)33-57(46(40)62)13-4-5-39-32-58(56-55-39)14-16-68-18-20-70-22-24-72-26-28-74-30-29-73-27-25-71-23-21-69-19-17-67-15-12-50-43(59)35-75-36-44(60)53-41(6-2-3-11-49)45(61)52-38-9-7-37(8-10-38)34-76-48(63)64/h7-10,31-32,41H,2-6,11-30,33-36,49H2,1H3,(H,50,59)(H,52,61)(H,53,60)(H,63,64)/t41-/m0/s1
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| InChIKey |
DAYAEKQIJOFUKD-RWYGWLOXSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1111.239
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Polar area
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353.86
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Complexity
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2207.668393
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xlogp Value
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-0.2271
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Heavy Count
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77
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Rot Bonds
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45
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Hbond acc
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23
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Hbond Donor
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5
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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
CN112341521B+ADC-5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC54) |
20.44 ug/mL
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| Method Description |
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (54%% inhibitory concentration).
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| In Vitro Model | Lung adenocarcinoma | HCC-827 cells | CVCL_2063 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC53) |
1181 ug/mL
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| Method Description |
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (53%% inhibitory concentration).
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| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC52) |
64.44 ug/mL
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| Method Description |
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (52%% inhibitory concentration).
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| In Vitro Model | Lung adenocarcinoma | NCI-H1650 cells | CVCL_1483 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC51) |
25.96 ug/mL
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| Method Description |
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (51%% inhibitory concentration).
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| In Vitro Model | Squamous cell carcinoma of the oral tongue, Tongue squamous cell carcinoma | CAL33 cells | CVCL_1108 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.69 ug/mL
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| Method Description |
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (50%% inhibitory concentration).
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| In Vitro Model | Hypopharyngeal squamous cell carcinoma | FaDu cells | CVCL_1218 | ||
References